Rapamycin (Synonyms: 雷帕霉素; 西罗莫司; Sirolimus; AY-22989)

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Rapamycin (Sirolimus) 是一种有效且特异性的 mTOR 抑制剂，作用于 HEK293 细胞，抑制 mTOR，IC₅₀ 为 0.1 nM。Rapamycin 与 FKBP12 结合且抑制 mTORC1。Rapamycin 还是一种自噬 (autophagy) 激活剂，免疫抑制剂。

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Rapamycin Chemical Structure

CAS No. : 53123-88-9

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10 mM * 1 mL in DMSO	￥605	In-stock
5 mg	￥343	In-stock
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Other Forms of Rapamycin:

MCE 顾客使用本产品发表的 890 篇科研文献

IHC

: Rapamycin purchased from MCE. Usage Cited in: J Hazard Mater. 2023 Jul 5,453,131354.; Rapamycin (50 nM; 24 h) partially reverses the cobalt-induced increase in LC3B-II and p62 levels in H4 cells.

: Rapamycin purchased from MCE. Usage Cited in: J Hazard Mater. 2023 Jul 5,453,131354.; Rapamycin (50 nM; 24 h) efficiently inhibits the Cobalt-induced hyperphosphorylation of Tau in Ser262 and Thr181, when in H4 cells.

: Rapamycin purchased from MCE. Usage Cited in: PLoS Pathog. 2023 Mar 27;19(3):e1011295. [Abstract]; Rapamycin (100 nM; 24 h) increases PRRSV replication in Marc-145 cells.

: Rapamycin purchased from MCE. Usage Cited in: Cancer Cell Int. 2023 Apr 16;23(1):68. [Abstract]; Rapamycin (2.5 mM; 24 h) ignificantly reverses the PCK1-sh-induced decreased expression of LC3B-II in SW480-sh cells.

: Rapamycin purchased from MCE. Usage Cited in: Cell Death Dis. 2020 Jun 12;11(6):454. [Abstract]; Immunofluorescence staining of p62 is conducted in HSC-T6 cells. G-Rg3 pretreatment with 16 μM and Ra are conducted with 100 or 200 nM.

: Rapamycin purchased from MCE. Usage Cited in: Nature. 2018 Jun;558(7711):540-546. [Abstract]; Western blot and quantification of P-AKT (Ser⁴⁷³) and P-S6RP in the liver, heart and muscle, respectively, of PIK3CA^WT and PIK3CA^CAGG-CreER mice treated with vehicle or Rapamycin directly after Cre induction.

: Rapamycin purchased from MCE. Usage Cited in: Acta Biomater. 2018 Nov;81:278-292. [Abstract]; Evident LC3 turnover and increased level of Atg5 are found upon Rapamycin treatment, which indicate significant autophagy activation.

: Rapamycin purchased from MCE. Usage Cited in: Int J Cancer. 2018 Aug 15;143(4):931-943. [Abstract]; H1975 cells are pretreated with Rapamycin (100 nM) for 1 h and then cells are exposed to IFN-γ (100 U/mL). Phosphorylation of AKT, S6, 4E-BP1 are analyzed by western blotting.

: Rapamycin purchased from MCE. Usage Cited in: Sci Rep. 2018 Mar 7;8(1):4108. [Abstract]; L02 cells exposed to PA (200 μM) with different concentrations of Rapamycin (Rapa) or Chloroquine (CQ) for 24 h. Palmitate (PA) induced higher protein expression of LC3 II/I and p62 compared with control as indicated by western blot.

: Rapamycin purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155. [Abstract]; Raw264.7 macrophages treated without or with Rapamycin (1 μΜ) or Chloroquine (20 μΜ) for 48 h. Western blot shows the protein expression levels of Atg5, Beclin1, LC3, and p62/SQSMT1.

: Rapamycin purchased from MCE. Usage Cited in: Pharmacol Biochem Behav. 2019 Feb;177:1-11. [Abstract]; Effect of treatment with Rapamycin, trehalose, or their combination on tyrosine hydroxylase (TH) expression in the striatum in MPTP-induced mouse model of Parkinson’s disease.

: Rapamycin purchased from MCE. Usage Cited in: Pharmacol Biochem Behav. 2019 Feb;177:1-11. [Abstract]; Effect of treatment with Rapamycin, trehalose, or their combination on autophagy activity measured by quantified immunoreactivity of LC3-II in the s. nigra. MPTP is administered at the dose of 20 mg/kg (i.p., daily) for 4 days to induce PD-like pathology.

: Rapamycin purchased from MCE. Usage Cited in: Biotechnol Appl Biochem. 2018 Sep;65(5):665-671. [Abstract]; The mTOR inhibitor Rapamycin augments the autophagy induced by GEM. (A, B) Beclin-1 and LC3B expression is analyzed by western blot after treatment of the cells with GEM (5 μM) and Rapamycin (0, 1, and 2.5 μM) for 48 (A) or 72 (B) h.

: Rapamycin purchased from MCE. Usage Cited in: PeerJ. 2018 Nov 21;6:e5988. [Abstract]; C6/36 cells are treated with 3-MA, Rapa or CQ for 36 h, 6 h and 36 h, respectively. For Rapa plus CQ treatment, C6/36 cells are treated with CQ for 30 h then treated with Rapa for 6 h. Mock and DMSO treated C6/36 cells are used as controls. After the treatment, the levels of AaAtg8-I and AaAtg8-II are analysed by immunoblotting using antibody against AaAtg8.

: Rapamycin purchased from MCE. Usage Cited in: PeerJ. 2018 Nov 21;6:e5988. [Abstract]; C6/36 cells are treated with 3-MA, Rapa or CQ for 36 h, 6 h and 36 h, respectively and then subjected to MDC staining. Mock and DMSO treated C6/36 cells are used as controls.

: Rapamycin purchased from MCE. Usage Cited in: Int J Ophthalmol. 2018 May 18;11(5):712-718. [Abstract]; Western blotting shows that Rapamycin treatment downregulates p-mTOR protein levels in infected and uninfected corneal tissues compared to the vehicle group.

: Rapamycin purchased from MCE. Usage Cited in: Evid Based Complement Alternat Med. 2018 Jun 26;2018:6049498. [Abstract]; Western blot analysis of AKT, p-Akt, mTOR, p-mTOR, FOXO1 and p-FOXO1 expression in U-87 MG cells after treatment with LY294002 (20 μM), Rapamycin (50 nM) or NAC (5 mM) with or without Xihuang pill (XHP).

: Rapamycin purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336. [Abstract]; Cells are pretreated with 5 mM 3-MA or 2 μM for 1 h and then exposed to 40 μM EPA and 10 μM Rp for 48 h. Cell extracts are prepared and subjected to western blot analysis.

: Rapamycin purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336. [Abstract]; Cells are treated with Rapamycin (Rp; 10 μM)+Eicosapentaenoic acid (EPA; 40 μM) with or without Chloroquine (CQ; 5 μM) for 48 h. Cell extracts are prepared and subjected to western blot analysis.

: Rapamycin purchased from MCE. Usage Cited in: J Clin Invest. 2017 Sep 1;127(9):3339-3352. [Abstract]; Phosphorylation of SMAD1/5/8 and SMAD2/3 in FOP-iMSCs. Serum-starved FOP-iMSCs are pretreated with 10 nM Rapamycin (Rapa), 1 μM DMH1, or 1 μM SB-431542 for 1 hour.

: Rapamycin purchased from MCE. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617. [Abstract]; Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitors Rapamycin, AZD2014, MLN0128, BEZ235 and 4EGI-1. Images are cropped for clarity from the same exposure of the same membrane.

: Rapamycin purchased from MCE. Usage Cited in: PLoS One. 2017 Nov 29;12(11):e0188748. [Abstract]; FTY720 reverses activation of autophagy induced by mTOR inhibitor, rapamycin. The impact of FTY720 and Rapamycin on the expression of Beclin1 and LC3 is evaluated by western blotting. Results are representative of 4 independent experiments.

: Rapamycin purchased from MCE. Usage Cited in: PLoS One. 2017 Jun 21;12(6):e0179772. [Abstract]; RAW264.7 cells transfected with miR-144-3p control or miR-144-3p mimic in full medium with or without 50μg/mL Rapamycin or 0.1% DMSO. 50 μg of total cell extracts are analyzed by Western blotting with a mouse anti-SQSTM1/p62 antibody. The p62 levels are detected by Western-blot (upper). Quantitative analysis of the p62 band normalized to β-actin is shown (lower).

: Rapamycin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2016 Dec 15;122:42-61. [Abstract]; Inhibition of SREBPs processing by AHI is dependent on LKB-1/AMPK/mTOR pathway. (A) HepG2 cells are incubated with or without MHY1485 or Rapamycin for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI. (B) HepG2 cells are incubated with or without Compound C for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI.

: Rapamycin purchased from MCE. Usage Cited in: Sci Bull. 2015 Dec;60(24):2120-2128.; CNE-2Z cells are treated with AZD8055 or Rapamycin with or without 1 T SMF for 3 d before they are harvested for Western blot.

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生物活性
纯度 & 产品资料
参考文献

生物活性

Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1^[1]. Rapamycin is an autophagy activator, an immunosuppressant^[2].

IC₅₀ & Target^[1]^[2]

mTOR

0.1 nM (IC₅₀, in HEK293 cells )

Microbial Metabolite

Autophagy

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	18.74 μM Compound: Rapamycin	Antiproliferative activity against human A549 cells by MTT assay Antiproliferative activity against human A549 cells by MTT assay	[PMID: 31546197]
A549	IC₅₀	30.72 μM Compound: Rapamycin	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33862514]
A549	IC₅₀	49.35 μM Compound: Rapamycin	Antitumor activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer-Glo assay Antitumor activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer-Glo assay	[PMID: 35688004]
HEK293	EC₅₀	0.05 μM Compound: Rapamycin	Inhibition of TPA-induced degradation of Pdcd4 (amino acid 39-91) expressed in human HEK293 cells assessed as minimum compound concentration required for 50% recovery of Pdcd4-luciferase signal incubated for 8 hrs by luciferase reporter gene assay Inhibition of TPA-induced degradation of Pdcd4 (amino acid 39-91) expressed in human HEK293 cells assessed as minimum compound concentration required for 50% recovery of Pdcd4-luciferase signal incubated for 8 hrs by luciferase reporter gene assay	[PMID: 21539301]
HEK293	IC₅₀	0.1 nM Compound: rapamycin	Inhibition of mTOR kinase expressed in human HEK293 cells by Western blot analysis Inhibition of mTOR kinase expressed in human HEK293 cells by Western blot analysis	[PMID: 17350953]
HEK-293T	EC₅₀	0.1 nM Compound: RAPA	Antiviral activity against HIV1 R5 assessed as inhibition of cell-cell fusion between R5-envelope expressing HEK293T cells and CD8 depleted human PBMCs pretreated for 6 days Antiviral activity against HIV1 R5 assessed as inhibition of cell-cell fusion between R5-envelope expressing HEK293T cells and CD8 depleted human PBMCs pretreated for 6 days	[PMID: 17485501]
HEK-293T	EC₅₀	1.3 nM Compound: RAPA	Antiviral activity against HIV1 X4 assessed as inhibition of cell-cell fusion between X4-envelope expressing HEK293T cells and CD8 depleted human PBMCs pretreated for 6 days Antiviral activity against HIV1 X4 assessed as inhibition of cell-cell fusion between X4-envelope expressing HEK293T cells and CD8 depleted human PBMCs pretreated for 6 days	[PMID: 17485501]
HeLa	IC₅₀	> 10000 nM Compound: Rapamycin	Growth inhibition of human HeLa cells after 72 hrs by CCK8 assay Growth inhibition of human HeLa cells after 72 hrs by CCK8 assay	[PMID: 29308895]
HepG2	EC₅₀	10 μM Compound: Sirolimus	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis	[PMID: 20966043]
HepG2	CC₅₀	67.2 μM Compound: 78	Cytotoxicity against human HepG2 assessed as reduction in cell viability after 24 hrs by CellTiter-Glo luminescent assay Cytotoxicity against human HepG2 assessed as reduction in cell viability after 24 hrs by CellTiter-Glo luminescent assay	[PMID: 28051303]
MCF7	EC₅₀	< 1 nM Compound: Rapamycin	Cytotoxicity against human MCF7 cells after 5 days by Presto blue reagent-based fluorescence analysis Cytotoxicity against human MCF7 cells after 5 days by Presto blue reagent-based fluorescence analysis	10.1039/C5MD00493D
MCF7	IC₅₀	18.74 μM Compound: Rapamycin	Antiproliferative activity against human MCF7 cells by MTT assay Antiproliferative activity against human MCF7 cells by MTT assay	[PMID: 31546197]
MCF7	IC₅₀	4980 nM Compound: Rapamycin	Growth inhibition of human MCF7 cells after 72 hrs by CCK8 assay Growth inhibition of human MCF7 cells after 72 hrs by CCK8 assay	[PMID: 29308895]
MDA-MB-231	GI₅₀	> 100 nM Compound: Rapamycin	Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 32510949]
MDA-MB-231	IC₅₀	> 10000 nM Compound: Rapamycin	Growth inhibition of human MDA-MB-231 cells after 72 hrs by CCK8 assay Growth inhibition of human MDA-MB-231 cells after 72 hrs by CCK8 assay	[PMID: 29308895]
MDA-MB-231	IC₅₀	0.9 μM Compound: Rapamycin	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
MDA-MB-231	IC₅₀	35.79 μM Compound: Rapamycin	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33862514]
MDA-MB-453	GI₅₀	0.05 nM Compound: Rapamycin	Antiproliferative activity against human MDA-MB-453 cells incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human MDA-MB-453 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 32510949]
MDA-MB-468	IC₅₀	37.2 μM Compound: Rapamycin	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33862514]
MEF	IC₅₀	0.05 nM Compound: Sirolimus	Inhibition of mTOR in mouse TSC1-/- MEF cells assessed as inhibition of S6 Ser240/244 phosphorylation incubated for 2 hrs by fluorescence based assay Inhibition of mTOR in mouse TSC1-/- MEF cells assessed as inhibition of S6 Ser240/244 phosphorylation incubated for 2 hrs by fluorescence based assay	[PMID: 31223435]
MV4-11	IC₅₀	> 500 nM Compound: RAPA	Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay	[PMID: 30629434]
NCI-H460	IC₅₀	> 10000 nM Compound: Rapamycin	Growth inhibition of human H460 cells after 72 hrs by CCK8 assay Growth inhibition of human H460 cells after 72 hrs by CCK8 assay	[PMID: 29308895]
OCI-AML2	IC₅₀	> 500 nM Compound: RAPA	Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay	[PMID: 30629434]
OCI-AML-3	IC₅₀	> 500 nM Compound: RAPA	Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay	[PMID: 30629434]
OVCAR-5	IC₅₀	> 10000 nM Compound: Rapamycin	Growth inhibition of human OVCAR5 cells after 72 hrs by CCK8 assay Growth inhibition of human OVCAR5 cells after 72 hrs by CCK8 assay	[PMID: 29308895]
PC-3	EC₅₀	43.1 μM Compound: Rapamycin	Cytotoxicity against human PC3 cells by MTT assay Cytotoxicity against human PC3 cells by MTT assay	[PMID: 28774426]
SiHa	IC₅₀	1756 nM Compound: Rapamycin	Growth inhibition of human SiHa cells after 72 hrs by CCK8 assay Growth inhibition of human SiHa cells after 72 hrs by CCK8 assay	[PMID: 29308895]
SK-OV-3	IC₅₀	> 10000 nM Compound: Rapamycin	Growth inhibition of human SKOV3 cells after 72 hrs by CCK8 assay Growth inhibition of human SKOV3 cells after 72 hrs by CCK8 assay	[PMID: 29308895]
SUM185PE	GI₅₀	0.04 nM Compound: Rapamycin	Antiproliferative activity against human SUM185PE cells incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human SUM185PE cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 32510949]
T47D	IC₅₀	1576 nM Compound: Rapamycin	Growth inhibition of human T47D cells after 72 hrs by CCK8 assay Growth inhibition of human T47D cells after 72 hrs by CCK8 assay	[PMID: 29308895]

体外研究
(In Vitro)

Rapamycin（12.5-100 nM；24 小时）处理在所有测试的细胞系（A549、SPC-A-1、95D 和 NCI-H446 细胞）中以剂量依赖性方式对肺癌细胞增殖产生适度抑制作用，达到约 100 nM 时细胞增殖减少 30-40%，而 12.5 nM 时减少约 10%^[3]。
将肺癌细胞系 95D 细胞单独或联合暴露于 Rapamycin（10 nM、20 nM）和 RP-56976（1 nM、10 nM）（Rapamycin 20 nM + RP-56976 10 nM）。单独暴露于 Rapamycin 或 RP-56976 24 小时后，不会显着改变 ERK1/2 的表达或磷酸化水平，而 Rapamycin 与 RP-56976 联合处理的细胞表现出 ERK1/2 磷酸化水平的显着降低^[3]。

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

Cell Viability Assay^[3]

Cell Line:	Lung cancer cell lines A549, SPC-A-1, 95D and NCI-H446
Concentration:	12.5 nM, 25 nM, 50 nM, 100 nM
Incubation Time:	24 hours
Result:	Treatment exerted modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines.

Western Blot Analysis^[3]

Cell Line:	95D cells
Concentration:	10 nM and 20 nM
Incubation Time:	24 hours
Result:	Combination treatment with RP-56976 decreased phosphorylation of ERK.

体内研究
(In Vivo)

Rapamycin (2.0 mg/kg; 腹腔内注射; 每隔一天;28 天) 单独使用有中等的抑制作用。然而，与对照组、Rapamycin 组相比，二甲双胍联合 Rapamycin 对肿瘤生长的抑制作用明显增强^[4]。

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

Animal Model:	24 male nu/nu mice aged 4-5 week old (15-20 g)^[4]
Dosage:	2.0 mg/kg
Administration:	Intraperitoneal injection; every other day; 28 days
Result:	Had a moderate inhibitory effect in monotherapy group. The combination with Metformin exerted a significantly increased inhibition of tumor growth.

Clinical Trial

分子量

914.17

Formula

C₅₁H₇₉NO₁₃

CAS 号

53123-88-9

性状

固体

颜色

White to off-white

中文名称

雷帕霉素；西罗莫司

结构分类

初始来源

Rapamycin (Synonyms: 雷帕霉素; 西罗莫司; Sirolimus; AY-22989)

Customer Review

Other Forms of Rapamycin:

Rapamycin 相关抗体

MCE 顾客使用本产品发表的 890 篇科研文献

Rapamycin 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 mTOR 亚型特异性产品:

查看 Antibiotic 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Rapamycin 相关抗体: