(+)-JQ-1 (Synonyms: JQ1)

目录号: HY-13030 纯度: 99.90%: Data Sheet SDS COA 产品使用指南
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(+)-JQ-1 (JQ1) 是一种化学探针，是一种有效特异性的可逆 BET bromodomain 抑制剂，抑制 BRD4(1/2) 的 IC₅₀ 分别为 77 nM 和 33 nM。(+)-JQ-1 激活自噬 (autophagy)。

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(+)-JQ-1 Chemical Structure

CAS No. : 1268524-70-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥935	In-stock
5 mg	￥850	In-stock
10 mg	￥1100	In-stock
50 mg	￥2250	In-stock
100 mg	￥3600	In-stock
200 mg	￥4350	In-stock
500 mg	￥5920	In-stock
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5 g		询价

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Customer Review

Other Forms of (+)-JQ-1:

(R)-(-)-JQ1 Enantiomer In-stock
JQ-1 (carboxylic acid) In-stock

MCE 顾客使用本产品发表的 276 篇科研文献

IHC

: (+)-JQ-1 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2022 Nov 11;41(1):321. [Abstract]; The expression of BRD4 and MYC proteins are each downregulated by JQ1 (0.5 µM; 24 h) or panobinostat (PAN; 10 nM; 24 h) alone, and more profoundly by the combination of these two inhibitors in in MB HD-MB03 and D-283 cells.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Res. 2019 Jan 1;79(1):251-262. [Abstract]; Cleavage of PARP is assessed by western blotting with the treatment of JQ 1.

: (+)-JQ-1 purchased from MCE. Usage Cited in: EBioMedicine. 2019 Jun:44:419-430. [Abstract]; Immunoblots (IB) are done to detect γH2AX and DNA repair proteins, Ku80 and RAD51 using UAB-PA4 or UAB-PA16 tumors harvested from mice 24 h following final treatment. Quantitation by densitometry of results is shown below each IB image.

: (+)-JQ-1 purchased from MCE. Usage Cited in: EBioMedicine. 2019 Jun:44:419-430. [Abstract]; Panc1 or MiaPaCa2 cells are exposed to JQ1 (0.5, 1, 5, or 10 μM) for 48 h, and immunoblotted for γH2AX.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Eur J Pharm Biopharm. 2019 Jan:134:96-106. [Abstract]; Western blot of cleaved Caspase-3 and cleaved PARP-1 in AML cells with the treatment of NL101 and BMN673.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Eur J Pharm Biopharm. 2019 Jan:134:96-106. [Abstract]; Western blot analysis of p21 and G2/M regulatory molecules, cyclin B1, CDC2, p-CDC2 (Tyr-15) and CDC25A in the treatment of NL101 and BMN673.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cell. 2018 Sep 20;175(1):186-199.e19. [Abstract]; Cells are treated with EPZ-6438 (1 μM) or GSK126 (1 μM) for 6 days. Protein levels are analyzed by immunoblotting. Cells are treated with EPZ-6438 (1 μM), JQ1 (0.25 μM) alone or combination for 6 days. Protein levels are analyzed by immunoblotting.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 28:420:195-207. [Abstract]; Shh-Light 2 cells are transfected with Gli1 or Gli2 plasmids and the expression of proteins are analyzed by Western blot. Positive control JQ1, CBC and CBD inhibit Gli1 and Gli2 overexpression induced Gli luciferase activity, GDC-0499 and GANT61 have no effects.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 10:419:64-74. [Abstract]; ESCC cell lines are treated with 500 nM JQ1 for 48 h, whole cell lysates are analyzed by western blotting. The expressions of p21 and p27 are further upregulated by JQ1 concomitant with cell cycle arrest at G1 phase.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Oct 28:435:44-54. [Abstract]; H157, H1299, and HCT116 cells are harvested for preparation of whole-cell protein lysates and subsequent Western blotting to detect the indicated proteins.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]; The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.

: (+)-JQ-1 purchased from MCE. Usage Cited in: EMBO Mol Med. 2018 Apr;10(4). pii: e8163. [Abstract]; Western blot analysis of MYC and FGFR3 expression in lysates from MGH-U3 and RT112 cells treated with (+)-JQ1 (1 or 4 μM) for 48 h. Anti-actin antibody is used as a loading control. Pan-FGFR inhibitor, PD173074 (50 nM and 1 μM), and inactive enantiomer (-)-JQ1 (4 μM) are used as controls.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Oncogene. 2018 Aug;37(33):4611-4625. [Abstract]; The OVCA429 cells are subjected to Western blot analysis for the indicated proteins. ACTIN servea as a loading control.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Oncogene. 2018 Aug;37(33):4611-4625. [Abstract]; ARID1A Western blot analysis of ARID1A protein levels in the ES2 polyclonal ARID1A knockout clone and ES2/OVCA429 monoclonal ARID1A knockout clones.

: (+)-JQ-1 purchased from MCE. Usage Cited in: J Med Chem. 2018 Jan 25;61(2):504-513. [Abstract]; Protein degradation profile of VHL-based BET degraders. Sub-confluent HeLa cells are treated for 24 h with varying concentration of test compounds JQ1(Compound 3), I-BET726 (Compound 4). Protein extracts are separated by SDS-PAGE and then analyzed by Western blot. Proteins Brd4, Brd3, Brd2 and β-actin are probed for JQ1and I-BET726 with specific antibodies.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Oct:156:511-523. [Abstract]; Western blot detection of the p-TEFb component CDK9, Cyclin T1 and CDK9 phosphorylation on Thr186, as well as its downstream RNA poly II CTD and phosphate CTD after J-Lat 10.6 cells are treated with PR-957 in dose-dependent manner.

: (+)-JQ-1 purchased from MCE. Usage Cited in: J Mol Cell Cardiol. 2019 Feb:127:83-96. [Abstract]; The expression of EndMT-related proteins, VE-cadherin, CD31, vimentin, α-SMA and FSP1, were compared among Ctrl, JQ1(-), JQ1, TGF-β1, and TGF-β1+JQ1 groups in both HUVECs and MAECs.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Biol Ther. 2018 May 4;19(5):407-415. [Abstract]; NSCLC cells are treated with 0-8 μM JQ1 for 24h, then the whole-cell lysates are prepared and subjected to western blot assay.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Sci Rep. 2018 Aug 1;8(1):11554. [Abstract]; A549 cells are mock-treated (0.1% DMSO in culture medium) or treated with RVX-208 at 500 nM, PFI-1 at 500 nM, JQ1 at 300 nM, or with 300 nM (-)-JQ1, an inactive enantiomer of JQ1. The cells are then infected with Ad2 at 1 PFU/cell for 24 h. Viral hexon and penton base (PB) protein is detected by immunoblotting analysis.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Oncotarget. 2018 May 1;9(33):23003-23017. [Abstract]; The expression of MYC protein is markedly repressed in JQ1-treated ccRCC cells (2.5 and 5 μM) in comparison with that in mock cells. β-Actin is used as a loading control. Densitometry analyses using ImageJ software are performed.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Leukemia. 2017 Oct;31(10):2037-2047. [Abstract]; Immunoprecipitation with anti-BIM antibody illustrates the increased binding of BIM to BCL-2 after JQ1 treatment.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Aug 28:402:100-109. [Abstract]; Expression and activation statuses of signal proteins in three BRAFV600E-mutant colon cancer cell lines treated with either RG7204, JQ1, or their combination. Phosphorylation of CRAF and AKT is suppressed by JQ1 in RKO cells and possibly in Colo205 cells (green arrow heads).

: (+)-JQ-1 purchased from MCE. Usage Cited in: Genome Res. 2017 Nov;27(11):1830-1842. [Abstract]; Ki67 immunohistochemistry and H&E stained sections from representative xenograft per treatment arm. A marked decrease in the proliferation marker Ki67 is observed in xenografts treated with JQ1.

: (+)-JQ-1 purchased from MCE. Usage Cited in: J Cell Biochem. 2017 Aug;118(8):2182-2192. [Abstract]; JQ1 induces G0/G1 cell cycle arrest and apoptosis of chondrosarcoma cells via regulating p21, p27, Cyclin E2, and Cyclin D1 expression. (A and B) JQ1 regulates the expression of cell cycle regulators such as p21, p27, Cyclin E2, and Cyclin D1. SW 1353 and Hs 819.T cells are seeded into a 6-well plate for 72 h, then the cells are treated with different concentrations of JQ1 (JQ1#1: 200 nM; JQ1#2: 2 μM; JQ1#3: 20 μM) for another 24 h. Total cell lysate is used for the analysis of protein expressio

: (+)-JQ-1 purchased from MCE. Usage Cited in: Metabolism. 2016 Oct;65(10):1478-88. [Abstract]; The BRD4 protein level in the liver is significantly suppressed by force-feeding fructose or glucose with (+)-JQ1. Protein levels of Brd4 in the liver of mice force-fed with glucose or fructose, with or without (+)-JQ1. Quantification of protein levels is performed by normalization against the level of β-actin (n = 6).

: (+)-JQ-1 purchased from MCE. Usage Cited in: Mol Cancer Ther. 2016 Jun;15(6):1217-26. [Abstract]; JQ1-mediated c-MYC repression correlates with growth inhibition. BETi preferentially inhibit c-MYC protein expression in sensitive cell lines. JQ1-sensitive GP5D, HT29 and LIM1215 cells and JQ1-resistant KM12, SW480 and HuTu80 cells where treated with JQ1 (500 nM) for 2-24 hours and c-MYC protein expression determined by western blot.

: (+)-JQ-1 purchased from MCE. Usage Cited in: PLoS Pathog. 2016 Oct 20;12(10):e1005950. [Abstract]; Dose effect of JQ1 on HSV infection. Vero cells are treated with JQ1 at concentrations as indicated. HSV-1 or HSV-2 at 1 MOI are used. The samples are used for protein expression analysis by western blot.

: (+)-JQ-1 purchased from MCE. Usage Cited in: J Biol Chem. 2016 Nov 4;291(45):23756-23768. [Abstract]; BET inhibition blocks growth of TNBC cells without consistently downregulating MYC. Western blot analysis of MYC expression levels in TNBC cell lines treated for 24 hours with vehicle or 500 nM JQ1. Values on the western blot are relative to the vehicle-treated 1143 sample following normalization to β-actin.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2016 Dec;1859(12):1527-1537. [Abstract]; JQ1 treatment decreases β-catenin levels in HCT116 cells, but increases TAZ protein. When cells reach confluence, they are serum-starved overnight and pretreated with DMSO or JQ1 (500 nM) for 1 hour, followed by growth medium (containing 10% serum) stimulation for 24 hours.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

(+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, and reversible BET bromodomain inhibitor, with IC₅₀s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2))^[1]. (+)-JQ-1 also activates autophagy^[2].

IC₅₀ & Target^[1]

BRD4(BD1BD2)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
697	EC₅₀	0.09 μM Compound: 1; (+)-JQ1	Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
A-375	IC₅₀	7.5 μM Compound: (+)-JQ1	Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
A2780	IC₅₀	0.1 μM Compound: Chemical probe: JQ1	Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 3 days by XTT assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 3 days by XTT assay	[PMID: 28881656]
A549	EC₅₀	17 μM Compound: (+)-JQ1	Cytotoxicity against human A549 cells assessed as viable cells incubated for 23 hrs by alamar blue assay Cytotoxicity against human A549 cells assessed as viable cells incubated for 23 hrs by alamar blue assay	[PMID: 35007061]
A549	IC₅₀	1.67 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human A549 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human A549 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
A549	IC₅₀	13.1 μM Compound: (+)-JQ1	Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
A549	IC₅₀	18.28 μM Compound: (+)-JQ1; 1	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 37379621]
ASPC1	IC₅₀	3.39 μM Compound: JQ1	Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay	[PMID: 35500243]
BCPAP	IC₅₀	254 nM Compound: JQ1	Anti-proliferative activity against human BCPAP cells assessed as reduction in cell proliferation incubated for 72 hrs Anti-proliferative activity against human BCPAP cells assessed as reduction in cell proliferation incubated for 72 hrs	[PMID: 28981843]
BT-474	IC₅₀	1.7 μM Compound: Cpd X1; (+)-JQ1	Antiproliferative activity against human BT474 cells Antiproliferative activity against human BT474 cells	[PMID: 31421967]
BT-549	IC₅₀	3.89 μM Compound: (+)-JQ1; 1	Antiproliferative activity against human BT-549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells incubated for 72 hrs by MTT assay	[PMID: 37379621]
CAPAN-1	IC₅₀	0.45 μM Compound: (+)-JQ1	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
CAPAN-1	IC₅₀	0.58 μM Compound: (+)-JQ1	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay	[PMID: 35091172]
CAPAN-1	IC₅₀	0.8 μM Compound: Cpd X1; (+)-JQ1	Antiproliferative activity against human Capan1 cells Antiproliferative activity against human Capan1 cells	[PMID: 31421967]
CAPAN-1	IC₅₀	2.44 μM Compound: (+)-JQ1	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay	[PMID: 35091172]
CAPAN-1	IC₅₀	2.44 μM Compound: JQ-1	Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability after 4 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 34813314]
CAPAN-1	IC₅₀	24.1 μM Compound: (+)-JQ1	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay	[PMID: 35091172]
CAPAN-1	IC₅₀	8.6 μM Compound: (+)-JQ1	Anticancer activity against human CAPAN-1 cells Anticancer activity against human CAPAN-1 cells	[PMID: 34107385]
CFPAC-1	IC₅₀	0.35 μM Compound: (+)-JQ1	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
CFPAC-1	IC₅₀	1.56 μM Compound: (+)-JQ1	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay	[PMID: 35091172]
CFPAC-1	IC₅₀	1.56 μM Compound: JQ-1	Antiproliferative activity against human CFPAC-1 cells assessed as reduction in cell viability after 4 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 34813314]
CFPAC-1	IC₅₀	1.86 μM Compound: (+)-JQ1	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay	[PMID: 35091172]
CFPAC-1	IC₅₀	13.9 μM Compound: (+)-JQ1	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay	[PMID: 35091172]
CT26	IC₅₀	28.67 μM Compound: 1; JQ1	Antiproliferative activity against human CT26 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human CT26 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33862375]
CWR22R	IC₅₀	0.033 μM Compound: 1, JQ1	Antiproliferative activity against human 22Rv1 cells assessed as inhibition of cell growth incubated for 96 to 120 hrs by celltiter glo assay Antiproliferative activity against human 22Rv1 cells assessed as inhibition of cell growth incubated for 96 to 120 hrs by celltiter glo assay	[PMID: 34999525]
CWR22R	IC₅₀	0.071 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human 22Rv1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human 22Rv1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
CWR22R	IC₅₀	0.071 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human 22Rv1 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay Antiproliferative activity against human 22Rv1 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	[PMID: 29541371]
CWR22R	IC₅₀	0.63 μM Compound: (+)-JQ1	Cytotoxicity against human androgen-independent/androgen-responsive 22Rv1 cells assessed as cell viability incubated for 96 hrs by MTT assay Cytotoxicity against human androgen-independent/androgen-responsive 22Rv1 cells assessed as cell viability incubated for 96 hrs by MTT assay	[PMID: 38153295]
D283 Med	IC₅₀	0.06 μM Compound: 1a; JQ1	Antiproliferative activity against human D283 Med cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human D283 Med cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay	[PMID: 36898329]
D283 Med	IC₅₀	256 nM Compound: Chemical probe: JQ1	Anti-proliferative activity against human D283 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay Anti-proliferative activity against human D283 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay	[PMID: 24231268]
D283 Med	IC₅₀	316 nM Compound: Chemical probe: JQ1	Anti-proliferative activity against human D283 cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay Anti-proliferative activity against human D283 cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay	[PMID: 24231268]
D283 Med	IC₅₀	477 nM Compound: Chemical probe: JQ1	Anti-proliferative activity against human D283 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Anti-proliferative activity against human D283 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 24231268]
D283 Med	IC₅₀	> 1 μM Compound: Chemical probe: JQ1	Anti-proliferative activity against human D283 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Anti-proliferative activity against human D283 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 24231268]
DU-145	EC₅₀	> 2000 nM Compound: (+)-JQ1	Antiproliferative activity against AR-positive human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against AR-positive human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 36577036]
DU-145	IC₅₀	0.2 μM Compound: Cpd X1; (+)-JQ1	Antiproliferative activity against human DU145 cells Antiproliferative activity against human DU145 cells	[PMID: 31421967]
DU-145	IC₅₀	2.1 μM Compound: (+)-JQ1	Cytotoxicity against human DU-145 cells assessed as cell viability incubated for 96 hrs by MTT assay Cytotoxicity against human DU-145 cells assessed as cell viability incubated for 96 hrs by MTT assay	[PMID: 38153295]
DU-145	IC₅₀	2.52 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human DU145 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human DU145 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
DU-145	IC₅₀	2.52 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human DU145 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay Antiproliferative activity against human DU145 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	[PMID: 29541371]
Daoy	IC₅₀	544 nM Compound: Chemical probe: JQ1	Anti-proliferative activity against human Daoy cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay Anti-proliferative activity against human Daoy cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay	[PMID: 24231268]
Daoy	IC₅₀	> 1 μM Compound: Chemical probe: JQ1	Anti-proliferative activity against human Daoy cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Anti-proliferative activity against human Daoy cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 24231268]
Daoy	IC₅₀	> 1 μM Compound: Chemical probe: JQ1	Anti-proliferative activity against human Daoy cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Anti-proliferative activity against human Daoy cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 24231268]
Daoy	IC₅₀	> 1 μM Compound: Chemical probe: JQ1	Anti-proliferative activity against human Daoy cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay Anti-proliferative activity against human Daoy cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay	[PMID: 24231268]
GES1	IC₅₀	17.98 μM Compound: (+)-JQ1	Antiproliferative activity against human GES1 cells incubated for 72 hrs MTT assay Antiproliferative activity against human GES1 cells incubated for 72 hrs MTT assay	[PMID: 38749341]
HCCLM3	IC₅₀	0.4 μM Compound: JQ1	Antiproliferative activity against human HCCLM3 cells incubated for 120 hrs in presence of FK866 by MTT assay Antiproliferative activity against human HCCLM3 cells incubated for 120 hrs in presence of FK866 by MTT assay	[PMID: 38691889]
HCCLM3	IC₅₀	86.17 μM Compound: JQ1	Antiproliferative activity against human HCCLM3 cells incubated for 120 hrs by MTT assay Antiproliferative activity against human HCCLM3 cells incubated for 120 hrs by MTT assay	[PMID: 38691889]
HCT-116	IC₅₀	0.4 μM Compound: Cpd X1; (+)-JQ1	Antiproliferative activity against human HCT116 cells Antiproliferative activity against human HCT116 cells	[PMID: 31421967]
HCT-116	IC₅₀	2.03 μM Compound: (+)-JQ1	Antiproliferative activity against BRCA2-mutated human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against BRCA2-mutated human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
HCT-116	IC₅₀	3.07 μM Compound: (+)-JQ1; 1	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay	[PMID: 37379621]
HCT-116	IC₅₀	4.212 μM Compound: 1; JQ1	Antiproliferation activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferation activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33214826]
HEK-293T	IC₅₀	107 nM Compound: JQ1	Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
HEL	IC₅₀	0.069 μM Compound: 6; +-JQ-1	Antiproliferative activity against human HEL cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human HEL cells incubated for 48 hrs by CCK8 assay	[PMID: 37037787]
HFF	EC₅₀	> 2000 nM Compound: (+)-JQ1	Cytotoxicity against HFF cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Cytotoxicity against HFF cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 36577036]
HFL1	IC₅₀	0.29 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against HFL1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against HFL1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
HL-60	EC₅₀	0.2 μM Compound: (+)-JQ1	Induction of ATRA-induced human HL60 cell differentiation pretreated for 1 hr followed by ATRA addition measured after 3 days by Wright-Giemsa staining based microscopic analysis Induction of ATRA-induced human HL60 cell differentiation pretreated for 1 hr followed by ATRA addition measured after 3 days by Wright-Giemsa staining based microscopic analysis	[PMID: 28549889]
HL-60	GI₅₀	0.021 μM Compound: 15; (+)-JQ1	Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay	[PMID: 33275431]
HL-60	IC₅₀	0.06 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human HL60 cells after 72 hrs by CCK8 assay Antiproliferative activity against human HL60 cells after 72 hrs by CCK8 assay	[PMID: 26731490]
HL-60	IC₅₀	0.07 μM Compound: (+)-JQ1	Antiproliferative activity against human HL-60 cells incubated for 72 hrs CCK-8 assay Antiproliferative activity against human HL-60 cells incubated for 72 hrs CCK-8 assay	[PMID: 38749341]
HL-60	IC₅₀	0.11 μM Compound: (+)-JQ1	Antiproliferative activity against BRD4-sensitive human HL60 cells after 72 hrs by CCK8 assay Antiproliferative activity against BRD4-sensitive human HL60 cells after 72 hrs by CCK8 assay	[PMID: 28314513]
HL-60	IC₅₀	0.15 μM Compound: 6; +-JQ-1	Antiproliferative activity against human HL-60 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells incubated for 48 hrs by CCK8 assay	[PMID: 37037787]
HL-60	IC₅₀	0.16 μM Compound: 1; (+)-jQ1	Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK8 assay	[PMID: 32883643]
HL-60	IC₅₀	0.87 μM Compound: 2; JQ1	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability by MTT assay	[PMID: 31857846]
HL-60	IC₅₀	2.91 μM Compound: (+)-JQ-1	Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK-8 assay	[PMID: 31079968]
HL-60	IC₅₀	3.46 μM Compound: (+)-JQ-1	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 32631570]
HL-60	IC₅₀	5.3 μM Compound: 3; (+)-JQ1	Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27266999]
HT-29	IC₅₀	0.02 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human HT-29 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human HT-29 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
HT-29	IC₅₀	0.104 μM Compound: 1, (+)-JQ1	Growth inhibition of human HT-29 cells after 72 hrs by SRB assay Growth inhibition of human HT-29 cells after 72 hrs by SRB assay	[PMID: 25559428]
HT-29	IC₅₀	0.28 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human HT-29 cells after 72 hrs by CCK8 assay Antiproliferative activity against human HT-29 cells after 72 hrs by CCK8 assay	[PMID: 26731490]
HT-29	IC₅₀	0.48 μM Compound: 1; (+)-jQ1	Antiproliferative activity against human HT29 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HT29 cells incubated for 72 hrs by MTT assay	[PMID: 32883643]
HT-29	IC₅₀	19.6 μM Compound: (+)-JQ1	Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
HT-29	IC₅₀	4.58 μM Compound: (+)-JQ1	Antiproliferative activity against human HT-29 cells incubated for 72 hrs MTT assay Antiproliferative activity against human HT-29 cells incubated for 72 hrs MTT assay	[PMID: 38749341]
HUVEC	IC₅₀	0.58 μM Compound: 6; +-JQ-1	Cytotoxicity against HUVECs assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Cytotoxicity against HUVECs assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 37037787]
HeLa	IC₅₀	3.76 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human HeLa cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human HeLa cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
HeLa	IC₅₀	> 100 μM Compound: 1, (+)-JQ1	Cytotoxicity against human HeLa cells after 24 hrs by WST-1 assay Cytotoxicity against human HeLa cells after 24 hrs by WST-1 assay	[PMID: 23517011]
Hep 3B2	IC₅₀	1.55 μM Compound: JQ1	Synergistic antiproliferative activity against human Hep3B cells measured after 72 hrs in presence of FK866 Synergistic antiproliferative activity against human Hep3B cells measured after 72 hrs in presence of FK866	[PMID: 38691889]
Hep 3B2	IC₅₀	5 μM Compound: JQ1	Antiproliferative activity against human Hep3B cells incubated for 120 hrs by MTT assay Antiproliferative activity against human Hep3B cells incubated for 120 hrs by MTT assay	[PMID: 38691889]
Hep 3B2	IC₅₀	5 μM Compound: JQ1	Antiproliferative activity against human Hep3B cells measured after 72 hrs Antiproliferative activity against human Hep3B cells measured after 72 hrs	[PMID: 38691889]
HepG2	IC₅₀	11.3 μM Compound: (+)-JQ1	Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
HepG2	IC₅₀	18.39 μM Compound: 1; JQ1	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33862375]
Hs-578T	IC₅₀	0.16 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human Hs578T cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human Hs578T cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
Huh-7	IC₅₀	0.67 μM Compound: JQ1	Antiproliferative activity against human Huh-7 cells incubated for 120 hrs in presence of FK866 by MTT assay Antiproliferative activity against human Huh-7 cells incubated for 120 hrs in presence of FK866 by MTT assay	[PMID: 38691889]
Huh-7	IC₅₀	62.85 μM Compound: JQ1	Antiproliferative activity against human Huh-7 cells incubated for 120 hrs by MTT assay Antiproliferative activity against human Huh-7 cells incubated for 120 hrs by MTT assay	[PMID: 38691889]
Jurkat	IC₅₀	16.29 μM Compound: (+)-JQ-1	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37992518]
K562	IC₅₀	0.64 μM Compound: 2; (+-)JQ1	Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay	[PMID: 27142751]
K562	IC₅₀	1.4 μM Compound: 6; +-JQ-1	Antiproliferative activity against human K562 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human K562 cells incubated for 48 hrs by CCK8 assay	[PMID: 37037787]
K562	IC₅₀	9.12 μM Compound: (+)-JQ1	Antiproliferative activity against BRD4-independent human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity against BRD4-independent human K562 cells after 72 hrs by CCK8 assay	[PMID: 28314513]
K562	IC₅₀	> 2 μM Compound: Chemical Probe: JQ1	Antiproliferative activity against human K562 cells assessed as decrease in cell viability after 96 hrs by WST-1 assay Antiproliferative activity against human K562 cells assessed as decrease in cell viability after 96 hrs by WST-1 assay	[PMID: 24403256]
K562	IC₅₀	> 2000 nM Compound: 1, JQ-1	Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
L02	IC₅₀	54.2 μM Compound: (+)-JQ1	Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay	[PMID: 30926312]
LNCaP	EC₅₀	162 nM Compound: (+)-JQ1	Antiproliferative activity against androgen-sensitive human LNCaP cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against androgen-sensitive human LNCaP cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 36577036]
LNCaP	IC₅₀	0.05 μM Compound: (+)-JQ1	Cytotoxicity against human AR-dependent LNCaP cells assessed as cell viability incubated for 96 hrs by MTT assay Cytotoxicity against human AR-dependent LNCaP cells assessed as cell viability incubated for 96 hrs by MTT assay	[PMID: 38153295]
LNCaP	IC₅₀	0.16 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human LNCAP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human LNCAP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
LNCaP	IC₅₀	0.16 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human LNCAP cells after 96 hrs by Cell-Titer glo reagent based luminescence assay Antiproliferative activity against human LNCAP cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	[PMID: 29541371]
LNCaP	IC₅₀	109.6 nM Compound: 1; (+)-JQ-1	Antiproliferative activity against human LNCAP cells Antiproliferative activity against human LNCAP cells	[PMID: 29758518]
LNCaP C4-2B	IC₅₀	0.19 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human C4-2B cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human C4-2B cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
LNCaP C4-2B	IC₅₀	0.19 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human C4-2B cells after 96 hrs by Cell-Titer glo reagent based luminescence assay Antiproliferative activity against human C4-2B cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	[PMID: 29541371]
LOUCY	EC₅₀	0.09 μM Compound: 1; (+)-JQ1	Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
LX-2	IC₅₀	< 0.032 μM Compound: JQ1	Antiproliferative activity against human LX2 cells incubated for 120 hrs by MTT assay Antiproliferative activity against human LX2 cells incubated for 120 hrs by MTT assay	[PMID: 38691889]
LX-2	IC₅₀	< 0.032 μM Compound: JQ1	Antiproliferative activity against human LX2 cells incubated for 120 hrs in presence of FK866 by MTT assay Antiproliferative activity against human LX2 cells incubated for 120 hrs in presence of FK866 by MTT assay	[PMID: 38691889]
MCF7	GI₅₀	> 50 μM Compound: 15; (+)-JQ1	Growth inhibition of human MCF7 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay Growth inhibition of human MCF7 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay	[PMID: 33275431]
MCF7	IC₅₀	0.2 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human MCF7 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human MCF7 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
MCF7	IC₅₀	12 μM Compound: JQ1	Anti-proliferative activity against human MCF7 cells assessed as reduction in cell proliferation incubated for 72 hrs Anti-proliferative activity against human MCF7 cells assessed as reduction in cell proliferation incubated for 72 hrs	[PMID: 28981843]
MCF7	IC₅₀	38 μM Compound: (+)-JQ1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
MCF7:CFR	IC₅₀	90 nM Compound: 1; JQ1	Growth inhibition of fulvestrant-resistant human MCF7:CFR cells measured after 5 days by Hoechst 33342 dye based imaging analysis Growth inhibition of fulvestrant-resistant human MCF7:CFR cells measured after 5 days by Hoechst 33342 dye based imaging analysis	[PMID: 32453591]
MDA-MB-231	IC₅₀	0.64 μM Compound: (+)-JQ1	Antiproliferative activity against BRCA-proficient human MDA-MB-231 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against BRCA-proficient human MDA-MB-231 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
MDA-MB-231	IC₅₀	0.64 μM Compound: JQ-1	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 7 days Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 7 days	[PMID: 34813314]
MDA-MB-231	IC₅₀	0.896 μM Compound: 6; JQ1	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay	[PMID: 38070430]
MDA-MB-231	IC₅₀	29.51 μM Compound: 1; JQ1	Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay	[PMID: 34908415]
MDA-MB-231	IC₅₀	3.148 μM Compound: JQ1; HY-13030	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37837671]
MDA-MB-231	IC₅₀	507 nM Compound: JQ1	Anti-proliferative activity against human MDA-MB-231 cells assessed as reduction in cell proliferation incubated for 72 hrs Anti-proliferative activity against human MDA-MB-231 cells assessed as reduction in cell proliferation incubated for 72 hrs	[PMID: 28981843]
MDA-MB-231	IC₅₀	6.17 μM Compound: (+)-JQ1; 1	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay	[PMID: 37379621]
MDA-MB-468	IC₅₀	0.54 μM Compound: (+)-JQ1	Antiproliferative activity against BRCA-proficient human MDA-MB-468 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against BRCA-proficient human MDA-MB-468 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
MDA-MB-468	IC₅₀	30.19 μM Compound: 1; JQ1	Antiproliferative activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay	[PMID: 34908415]
MM1.S	IC₅₀	0.019 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay	[PMID: 28586718]
MM1.S	IC₅₀	0.02 μM Compound: 2; (+)-JQ1	Cytotoxicity against human MM1S cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MM1S cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28535045]
MM1.S	IC₅₀	0.062 μM Compound: JQ1	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 36563515]
MM1.S	IC₅₀	0.109 μM Compound: 1, (+)-JQ1	Growth inhibition of human MM1S cells after 72 hrs by SRB assay Growth inhibition of human MM1S cells after 72 hrs by SRB assay	[PMID: 25559428]
MM1.S	IC₅₀	2.84 μM Compound: (+)-JQ-1	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37992518]
MM1.S	IC₅₀	29.8 nM Compound: (+)-JQ-1; 1	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay	[PMID: 31490070]
MM1.S	IC₅₀	33 nM Compound: JQ1	Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
MM1.S	IC₅₀	69.1 nM Compound: 1; (+)-JQ-1	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay	[PMID: 29525435]
MOLM-13	IC₅₀	0.024 μM Compound: 1a; JQ1	Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay	[PMID: 36898329]
MOLM-13	IC₅₀	1.73 μM Compound: (+)-JQ-1	Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37992518]
MOLM-13	IC₅₀	56 nM Compound: 1, JQ-1	Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
MOLM-13	IC₅₀	56 nM Compound: 1; JQ-1	Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay	[PMID: 28463487]
MV4-11	GI₅₀	0.08 μM Compound: (+)-JQ-1	Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay	[PMID: 26191363]
MV4-11	IC₅₀	0.012 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human MV4-11 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells after 72 hrs by CCK8 assay	[PMID: 26731490]
MV4-11	IC₅₀	0.017 μM Compound: 1, JQ1	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 96 to 120 hrs by celltiter glo assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 96 to 120 hrs by celltiter glo assay	[PMID: 34999525]
MV4-11	IC₅₀	0.023 μM Compound: 1, (+)-JQ1	Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay	[PMID: 25559428]
MV4-11	IC₅₀	0.042 μM Compound: JQ1	Antiproliferative activity against human MM4-11 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human MM4-11 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 36563515]
MV4-11	IC₅₀	0.06 μM Compound: Cpd X1; (+)-JQ1	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 31421967]
MV4-11	IC₅₀	0.08 μM Compound: (+)-JQ1	Antiproliferative activity against BRD4-sensitive human MV411 cells after 72 hrs by CCK8 assay Antiproliferative activity against BRD4-sensitive human MV411 cells after 72 hrs by CCK8 assay	[PMID: 28314513]
MV4-11	IC₅₀	0.08082 μM Compound: 1; JQ1	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay	[PMID: 31767403]
MV4-11	IC₅₀	0.099 μM Compound: 1a; JQ1	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay	[PMID: 36898329]
MV4-11	IC₅₀	0.14 μM Compound: (+)-JQ1	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs CCK-8 assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs CCK-8 assay	[PMID: 38749341]
MV4-11	IC₅₀	0.157 μM Compound: (+)-JQ-1	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo assay	[PMID: 34731760]
MV4-11	IC₅₀	0.16 μM Compound: (+)-JQ-1	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 32631570]
MV4-11	IC₅₀	0.16 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human MV4-11 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human MV4-11 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
MV4-11	IC₅₀	0.24 μM Compound: 2; (+-)JQ1	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay	[PMID: 27142751]
MV4-11	IC₅₀	0.242 μM Compound: 1, (+)-JQ1	Cytotoxicity against human MV4-11 cells after 72 hrs by MTS assay Cytotoxicity against human MV4-11 cells after 72 hrs by MTS assay	[PMID: 23517011]
MV4-11	IC₅₀	0.57 μM Compound: (+)-JQ-1	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK-8 assay	[PMID: 31079968]
MV4-11	IC₅₀	1.3 μM Compound: (+)-JQ-1	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37992518]
MV4-11	IC₅₀	24 nM Compound: 1, JQ-1	Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
MV4-11	IC₅₀	24 nM Compound: 1; JQ-1	Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay	[PMID: 28463487]
MV4-11	IC₅₀	6.4 μM Compound: 3; (+)-JQ1	Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27266999]
MV4-11	IC₅₀	72 nM Compound: (+)-JQ1	Anticancer activity against human MV4-11 cells assessed as cell growth inhibition Anticancer activity against human MV4-11 cells assessed as cell growth inhibition	[PMID: 32502863]
MV4-11	IC₅₀	72 nM Compound: 7; (+)-JQ1	Antiproliferative activity against human MV4-11 cells Antiproliferative activity against human MV4-11 cells	[PMID: 28195723]
MX1	EC₅₀	0.144 μM Compound: 1; (+)-JQ1	Inhibition of BRD4 in human MX1 cells assessed as decrease in cell proliferation after 3 days by Celltiter-Glo assay Inhibition of BRD4 in human MX1 cells assessed as decrease in cell proliferation after 3 days by Celltiter-Glo assay	[PMID: 31303996]
MX1	EC₅₀	254 nM Compound: 1b; JQ1	Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay	[PMID: 28949521]
Medulloblastoma cell	IC₅₀	~ 50 nM Compound: Chemical Probe: JQ1	Cytotoxicity in Ptch-mutated in human medulloblastoma cells expressing wildtype SMO by CellTiter-Glo analysis Cytotoxicity in Ptch-mutated in human medulloblastoma cells expressing wildtype SMO by CellTiter-Glo analysis	[PMID: 24973920]
Monocyte	IC₅₀	0.002 μM Compound: JQ-1	Inhibition of LPS-induced MCP-1 production in mouse Monocyte Inhibition of LPS-induced MCP-1 production in mouse Monocyte	[PMID: 38876177]
NALM-6	EC₅₀	0.06 μM Compound: 1; (+)-JQ1	Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
NCI-H1975	IC₅₀	1.23 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human NCI-H1975 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human NCI-H1975 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
NRK-49F	IC₅₀	21.1 μM Compound: (+)-JQ1	Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
OCI-AML-3	IC₅₀	~ 500 nM Compound: Chemical Probe: JQ1	Antiproliferative activity against human OCI-AML-3 cells harbouring DNMT3A-R882C and NPM1c mutants co-expressing wild-type p53 assessed as decrease in cell viability after 96 hrs by WST-1 assay Antiproliferative activity against human OCI-AML-3 cells harbouring DNMT3A-R882C and NPM1c mutants co-expressing wild-type p53 assessed as decrease in cell viability after 96 hrs by WST-1 assay	[PMID: 24403256]
ONS-76	IC₅₀	123 nM Compound: Chemical probe: JQ1	Anti-proliferative activity against human ONS-76 cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay Anti-proliferative activity against human ONS-76 cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay	[PMID: 24231268]
ONS-76	IC₅₀	172 nM Compound: Chemical probe: JQ1	Anti-proliferative activity against human ONS-76 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Anti-proliferative activity against human ONS-76 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 24231268]
ONS-76	IC₅₀	175 nM Compound: Chemical probe: JQ1	Anti-proliferative activity against human ONS-76 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay Anti-proliferative activity against human ONS-76 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay	[PMID: 24231268]
ONS-76	IC₅₀	87 nM Compound: Chemical probe: JQ1	Anti-proliferative activity against human ONS-76 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Anti-proliferative activity against human ONS-76 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 24231268]
OVCAR-3	IC₅₀	0.1 μM Compound: Chemical probe: JQ1	Cytotoxicity against human OVCAR-3 cells assessed as reduction in cell viability after 3 days by XTT assay Cytotoxicity against human OVCAR-3 cells assessed as reduction in cell viability after 3 days by XTT assay	[PMID: 28881656]
OVCAR-5	IC₅₀	0.1 μM Compound: Chemical probe: JQ1	Cytotoxicity against human OVCAR-5 cells assessed as reduction in cell viability after 3 days by XTT assay Cytotoxicity against human OVCAR-5 cells assessed as reduction in cell viability after 3 days by XTT assay	[PMID: 28881656]
OVCAR-8	IC₅₀	0.1 μM Compound: Chemical probe: JQ1	Cytotoxicity against human OVCAR-8 cells assessed as reduction in cell viability after 3 days by XTT assay Cytotoxicity against human OVCAR-8 cells assessed as reduction in cell viability after 3 days by XTT assay	[PMID: 28881656]
PC-3	EC₅₀	> 2000 nM Compound: (+)-JQ1	Antiproliferative activity against androgen-insensitive human PC-3 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against androgen-insensitive human PC-3 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 36577036]
PC-3	IC₅₀	1.28 μM Compound: (+)-JQ1	Cytotoxicity against human PC-3 cells assessed as cell viability incubated for 96 hrs by MTT assay Cytotoxicity against human PC-3 cells assessed as cell viability incubated for 96 hrs by MTT assay	[PMID: 38153295]
PC-3	IC₅₀	3.01 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human PC3 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human PC3 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
PC-3	IC₅₀	3.01 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human PC3 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay Antiproliferative activity against human PC3 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	[PMID: 29541371]
Raji	IC₅₀	0.069 μM Compound: 2, (+)-JQ1	Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs	[PMID: 24900758]
Raji	IC₅₀	~ 1 μM Compound: Chemical Probe: JQ1	Antiproliferative activity against human Raji cells assessed as decrease in cell viability after 96 hrs by WST-1 assay Antiproliferative activity against human Raji cells assessed as decrease in cell viability after 96 hrs by WST-1 assay	[PMID: 24403256]
SK-MEL-5	GI₅₀	> 40 μM Compound: 15; (+)-JQ1	Growth inhibition of human SK-MEL-5 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay Growth inhibition of human SK-MEL-5 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay	[PMID: 33275431]
SK-OV-3	IC₅₀	0.1 μM Compound: Chemical probe: JQ1	Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell viability after 3 days by XTT assay Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell viability after 3 days by XTT assay	[PMID: 28881656]
SW1990	IC₅₀	0.63 μM Compound: (+)-JQ1	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
SW1990	IC₅₀	1.11 μM Compound: (+)-JQ1	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 5 days by MTT assay	[PMID: 35091172]
SW1990	IC₅₀	3.74 μM Compound: (+)-JQ1	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 4 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 4 days by MTT assay	[PMID: 35091172]
SW1990	IC₅₀	3.74 μM Compound: JQ-1	Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability after 4 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 34813314]
SW1990	IC₅₀	31.6 μM Compound: (+)-JQ1	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth after 3 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth after 3 days by MTT assay	[PMID: 35091172]
SW480	IC₅₀	14.1 μM Compound: Cpd X1; (+)-JQ1	Antiproliferative activity against human SW480 cells Antiproliferative activity against human SW480 cells	[PMID: 31421967]
T-cell	IC₅₀	0.11 μM Compound: 6m; JQ1	Immunosuppressive activity in BALB/c mouse splenic T cells assessed as inhibition of PMA/CD28 induced cell proliferation after 24 hrs by [methyl-3H]thymidine incorporation assay Immunosuppressive activity in BALB/c mouse splenic T cells assessed as inhibition of PMA/CD28 induced cell proliferation after 24 hrs by [methyl-3H]thymidine incorporation assay	[PMID: 26869194]
THP-1	GI₅₀	15.5 μM Compound: JQ1(+)	Growth inhibition of human THP-1 cells Growth inhibition of human THP-1 cells	[PMID: 32320239]
THP-1	IC₅₀	0.33 μM Compound: (+)-JQ1	Antiproliferative activity against human THP-1 cells expressing BRD4 assessed as inhibition of cell growth measured after 3 days by MTT assay Antiproliferative activity against human THP-1 cells expressing BRD4 assessed as inhibition of cell growth measured after 3 days by MTT assay	[PMID: 35091172]
THP-1	IC₅₀	0.56 μM Compound: JQ-1	Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS-induced IL-6 production incubated for 18 hrs by ELISA Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS-induced IL-6 production incubated for 18 hrs by ELISA	[PMID: 35318165]
TPC1	IC₅₀	462 nM Compound: JQ1	Anti-proliferative activity against human TPC1 cells assessed as reduction in cell proliferation incubated for 72 hrs Anti-proliferative activity against human TPC1 cells assessed as reduction in cell proliferation incubated for 72 hrs	[PMID: 28981843]
U-266	IC₅₀	3.45 μM Compound: 1; JQ1	Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33862375]
U-937	IC₅₀	> 20 μM Compound: 3; (+)-JQ1	Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27266999]
U2OS	IC₅₀	1.62 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human U2OS cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human U2OS cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
U2OS	IC₅₀	> 100 μM Compound: 1, (+)-JQ1	Cytotoxicity against human U2OS cells after 24 hrs by WST-1 assay Cytotoxicity against human U2OS cells after 24 hrs by WST-1 assay	[PMID: 23517011]
VCaP	EC₅₀	160.3 nM Compound: (+)-JQ1	Antiproliferative activity against AR-positive human VCaP cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against AR-positive human VCaP cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 36577036]
VCaP	IC₅₀	0.012 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human VCaP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human VCaP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
WI-38	IC₅₀	4.97 μM Compound: 1; (+)-jQ1	Antiproliferative activity against human WI-38 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human WI-38 cells incubated for 72 hrs by MTT assay	[PMID: 32883643]

体外研究
(In Vitro)

(+)-JQ-1 代表溴结构域 BET 家族的一种有效、高度特异性和 Kac 竞争性抑制剂。(+)- JQ-1 (100 nM，48 h) 促进鳞状分化，表现为细胞纺锤形、扁平化和角蛋白表达增加。与 (-)-JQ1 (250 nM) 和载体对照相比，(+)-JQ-1 (250 nM) 在经处理的 NMC 797 细胞中诱导角蛋白的快速表达，如通过定量免疫组织化学所确定的。(+)-JQ-1 (与 (-)-JQ1 (250 nM) 相比) 会引发经处理的 NMC 797 细胞的时间依赖性强 (3+) 角蛋白染色^[1]。添加 (+)-JQ-1 后几乎立即观察到自噬基因的去抑制^[2]。(+)-JQ-1 是 BET 家族共激活蛋白 BRD4 的一种有效的噻吩二氮卓抑制剂 (K_d=90 nM)，通过 MYC 致癌基因的转录控制参与癌症的发病机制。(+)-JQ-1 的剂量范围研究证明有效抑制 H4Kac4 结合，小鼠 BRDT (1) 的 IC₅₀ 值为 10 nM，人 BRDT (1) 的 IC₅₀ 值为 11 nM^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

已确定肿瘤的匹配小鼠队列随机接受 (+)-JQ1 (50 mg/kg) 或载体处理，每日腹膜内注射。在随机化之前和处理四天之后，通过 FDG-PET 成像评估小鼠。(+)-JQ1 处理观察到 FDG 摄取显著减少。肿瘤体积测量证实 JQ1 处理可减少肿瘤生长。(+)-JQ1 的药代动力学研究是在 CD1 小鼠静脉内和口服给药后进行的。静脉内给药 (5 mg/kg) 后 (+)-JQ1 的平均血浆浓度-时间曲线。静脉内 (+)-JQ1 的药代动力学参数显示出出色的药物暴露 (AUC=2090 hr*ng/mL) 和大约一小时的半衰期 (T1/2)。制定口服给药 (10 mg/kg) 后 (+)-JQ1 的平均血浆浓度-时间曲线。口服 (+)-JQ1 的药代动力学参数表现出出色的口服生物利用度 (F=49%)、血浆峰浓度 (C_max=1180 ng/mL) 和药物暴露量 (AUC=2090 hr*ng)/mL)^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

456.99

Formula

C₂₃H₂₅ClN₄O₂S

CAS 号

1268524-70-4

性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 45 mg/mL (98.47 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1882 mL	10.9412 mL	21.8823 mL
5 mM	0.4376 mL	2.1882 mL	4.3765 mL
10 mM	0.2188 mL	1.0941 mL	2.1882 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.47 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.47 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.47 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 20% HP-β-CD in Saline
Solubility: 10 mg/mL (21.88 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 15% Cremophor EL 85% Saline
Solubility: 10 mg/mL (21.88 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.90%

选择批次：

Data Sheet (690 KB) SDS (393 KB)

COA (295 KB) HNMR (165 KB) LCMS (367 KB) 元素分析报告 (218 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. [Content Brief]

[2]. Sakamaki JI, et al. Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and LysosomalFunction. Mol Cell. 2017 May 18;66(4):517-532.e9. [Content Brief]

[3]. Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. Cell. 2012 Aug 17;150(4):673-84. [Content Brief]

Cell Assay ^[1]	NUT midline carcinoma patient cell lines (797 and 11060) are plated in T-25 flasks and grown in DMEM (797) or RPMI (11060) containing 10 % fetal bovine serum. Cells are treated with either 250 nM (+)-JQ1, 250 nM (-)-JQ1 or the equivalent volume of DMSO (0.025%). At the desired time point, 2×10⁶ cells are spun at 500× g for 5 minutes at 4°C and washed with PBS. Pellets are resuspended in 1 mL of cold PBS and added dropwise while gently vortexing to 9 mL 70 % ethanol in a 15 mL polypropylene centrifuge tube. Fixed cells are then frozen at -20°C overnight. The next day, cells are centrifuged at 500× g for 10 minutes at 4°C and washed with 3 mL of cold PBS. Cells are resuspended in 500 μL of propidium iodide staining solution (0.2 mg/mL RNAse A, 0.02 mg/mL propidium iodide, 0.1 % Triton-X in PBS) and incubated for 20 minutes at 37°C. Samples are then transferred to ice and analyzed on a BD FACS Canto II. Histograms are generated and cell cycle analysis is performed using FlowJo flow cytometry analysis software^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]^[3]	Mice^[1] Matched cohorts of mice with established tumors are randomized to treatment with (+)-JQ1 (50 mg/kg) or vehicle, administered by daily intraperitoneal injection. Male CD1 mice (24-29 g) are treated with a single dose of (+)-JQ1 at 5 mg/kg for intravenous tail vein injection studies and 10 mg/kg for oral gavage studies. Rats^[3] Adult male Sprague-Dawley rats are treated with vehicle or (+)-JQ1 (10 mg/kg). Treatment is administered IP at 1/100 body mass. Rats are checked twice-daily for mortality and weighed on days 1, 3, 7, 14, and 21. The treatment regimen utilized 4 days of 50 mg/kg JQ1 administered daily which is decreased to 10 mg/kg twice daily for the remainder of the study due to the appearance of adverse effects in a subset of animals. For all animals completing 3 weeks of treatment, testis mass, sperm motility, and sperm counts are determined as described for mouse studies. In brief, testes are fixed in Bouin’s and prepared for histology. The other half is minced in warm M16 buffer and used for sperm counts and motility studies. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. [Content Brief] [2]. Sakamaki JI, et al. Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and LysosomalFunction. Mol Cell. 2017 May 18;66(4):517-532.e9. [Content Brief] [3]. Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. Cell. 2012 Aug 17;150(4):673-84. [Content Brief]

(+)-JQ-1 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1882 mL	10.9412 mL	21.8823 mL	54.7058 mL
	5 mM	0.4376 mL	2.1882 mL	4.3765 mL	10.9412 mL
	10 mM	0.2188 mL	1.0941 mL	2.1882 mL	5.4706 mL
	15 mM	0.1459 mL	0.7294 mL	1.4588 mL	3.6471 mL
	20 mM	0.1094 mL	0.5471 mL	1.0941 mL	2.7353 mL
	25 mM	0.0875 mL	0.4376 mL	0.8753 mL	2.1882 mL
	30 mM	0.0729 mL	0.3647 mL	0.7294 mL	1.8235 mL
	40 mM	0.0547 mL	0.2735 mL	0.5471 mL	1.3676 mL
	50 mM	0.0438 mL	0.2188 mL	0.4376 mL	1.0941 mL
	60 mM	0.0365 mL	0.1824 mL	0.3647 mL	0.9118 mL
	80 mM	0.0274 mL	0.1368 mL	0.2735 mL	0.6838 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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