UNC0638

目录号: HY-15273 纯度: 99.48%: Data Sheet SDS COA 产品使用指南
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UNC0638 是一种化学探针，选择性抑制 G9a 和 GLP 组蛋白甲基转移酶，IC₅₀ 分别为 15 nM 和 19 nM。UNC0638 在体外可抑制 TNBC 细胞的侵袭和迁移。UNC0638 也是 EHMT1/2 的抑制剂，在人红细胞祖细胞培养中诱导胎儿血红蛋白 (HbF) 表达。此外，UNC0638 具有抗 FMDV (口蹄疫病毒) 和抗 VSV (水疱性口炎病毒) 的活性，对多种表观遗传和非表观遗传靶标具有出色的效力和选择性。

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UNC0638 Chemical Structure

CAS No. : 1255580-76-7

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥673	In-stock
1 mg	￥272	In-stock
5 mg	￥600	In-stock
10 mg	￥900	In-stock
25 mg	￥1800	In-stock
50 mg	￥2800	In-stock
100 mg	￥4200	In-stock
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Other Forms of UNC0638:

UNC0638 hydrate 询价

MCE 顾客使用本产品发表的 10 篇科研文献

: UNC0638 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.

: UNC0638 purchased from MCE. Usage Cited in: Mol Med Rep. 2018 Feb;17(2):2239-2244. [Abstract]; UNC0638 suppresses triple negative breast cancer cell migration and invasion by regulating EMT associated proteins. Western blots of EMT associated proteins.

UNC0638 相关产品

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查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

UNC0638, a chemical probe, selectively inhibits G9a and GLP histone methyltransferases with IC₅₀ of 15 nM and 19 nM, respectively. UNC0638 inhibits TNBC cell invasion and migration in vitro. UNC0638 is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets^[1]^[2]^[3]^[4]^[5].

IC₅₀ & Target

EHMT2/G9a/KMT1C

EHMT1/GLP/KMT1D

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CWR22R	EC₅₀	0.2 μM Compound: Chemical probe: UNC0638	Antiproliferative against human 22RV1 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human 22RV1 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
CWR22R	EC₅₀	4.5 μM Compound: 5, UNC0638	Cytotoxicity against human 22Rv1 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human 22Rv1 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
CWR22R	IC₅₀	0.048 μM Compound: 5, UNC0638	Inhibition of G9a in human 22Rv1 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human 22Rv1 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
Calu-1	EC₅₀	1.3 μM Compound: Chemical probe: UNC0638	Antiproliferative against human Calu-1 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human Calu-1 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
Calu-6	EC₅₀	1.5 μM Compound: Chemical probe: UNC0638	Antiproliferative against human Calu-6 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human Calu-6 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
DU-145	EC₅₀	0.7 μM Compound: Chemical probe: UNC0638	Antiproliferative against human DU-145 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human DU-145 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
Daoy	EC₅₀	0.1 μM Compound: Chemical probe: UNC0638	Antiproliferative against human Daoy cells after 7 days by Cell-Titer Glo assay Antiproliferative against human Daoy cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
G-401	EC₅₀	0.4 μM Compound: Chemical probe: UNC0638	Antiproliferative against human G-401 cells after 7 days by Cell-Titer Glo assay Antiproliferative against human G-401 cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
HCT-116	EC₅₀	11 μM Compound: 5, UNC0638	Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
HCT-116	EC₅₀	11 μM Compound: 5, UNC0638	Cytotoxicity against p53-deficient human HCT116 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against p53-deficient human HCT116 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
HCT-116	IC₅₀	0.21 μM Compound: 5, UNC0638	Inhibition of G9a in human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
HCT-116	IC₅₀	0.24 μM Compound: 5, UNC0638	Inhibition of G9a in p53-deficient human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in p53-deficient human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
HCT-116	IC₅₀	3.35 μM Compound: UNC0638	Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 72 hrs by MTT assay	[PMID: 27720557]
HFF	IC₅₀	2286 nM Compound: 19; UNC0638	Cytotoxicity against HFF Cytotoxicity against HFF	[PMID: 30366254]
HL-60	EC₅₀	6.5 μM Compound: Chemical probe: UNC0638	Antiproliferative against human HL-60 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human HL-60 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
HL-60	IC₅₀	23.75 μM Compound: Chemical Probe: UNC0638	Cytotoxicity against human HL-60 cells assessed as decrease in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human HL-60 cells assessed as decrease in cell viability measured after 48 hrs by MTT assay	[PMID: 25978433]
HL-60	IC₅₀	27.38 μM Compound: Chemical Probe: UNC0638	Cytotoxicity against human HL-60 cells assessed as decrease in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human HL-60 cells assessed as decrease in cell viability measured after 24 hrs by MTT assay	[PMID: 25978433]
HT-1080	EC₅₀	0.5 nM Compound: Chemical probe: UNC0638	Antiproliferative activity against human HT-1080 cells after 5 days by Cell-Titer-Glo assay Antiproliferative activity against human HT-1080 cells after 5 days by Cell-Titer-Glo assay	[PMID: 26147105]
HT-1080	EC₅₀	0.5 μM Compound: Chemical probe: UNC0638	Antiproliferative against human HT-1080 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human HT-1080 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
HT-1080	EC₅₀	1.2 nM Compound: Chemical probe: UNC0638	Antiproliferative activity against human HT-1080 cells after 2 days by Cell-Titer-Glo assay Antiproliferative activity against human HT-1080 cells after 2 days by Cell-Titer-Glo assay	[PMID: 26147105]
HepG2	IC₅₀	3.7 μM Compound: UNC0638	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by MTT assay	[PMID: 27720557]
IMR-32	EC₅₀	> 10 μM Compound: Chemical probe: UNC0638	Antiproliferative against human IMR-32 cells after 7 days by Cell-Titer Glo assay Antiproliferative against human IMR-32 cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
IMR-90	EC₅₀	2.3 μM Compound: 5, UNC0638	Cytotoxicity against human IMR90 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human IMR90 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
IMR-90	IC₅₀	0.12 μM Compound: 5, UNC0638	Inhibition of G9a in human IMR90 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human IMR90 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
K562	EC₅₀	5.3 μM Compound: Chemical probe: UNC0638	Antiproliferative against human K562 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human K562 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
KG-1a	IC₅₀	22.36 μM Compound: Chemical Probe: UNC0638	Cytotoxicity against human KG-1a cells assessed as decrease in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human KG-1a cells assessed as decrease in cell viability measured after 48 hrs by MTT assay	[PMID: 25978433]
KG-1a	IC₅₀	26.53 μM Compound: Chemical Probe: UNC0638	Cytotoxicity against human KG-1a cells assessed as decrease in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human KG-1a cells assessed as decrease in cell viability measured after 24 hrs by MTT assay	[PMID: 25978433]
KMS-11	EC₅₀	4 μM Compound: Chemical probe: UNC0638	Antiproliferative against human KMS-11 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human KMS-11 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
KMS-12-BM	EC₅₀	4.4 μM Compound: Chemical probe: UNC0638	Antiproliferative against human KMS-12-BM cells after 5 days by Cell-Titer Glo assay Antiproliferative against human KMS-12-BM cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
Kasumi 1	EC₅₀	1.1 μM Compound: Chemical probe: UNC0638	Antiproliferative against human Kasumi-1 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human Kasumi-1 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
L-363	EC₅₀	3.9 μM Compound: Chemical probe: UNC0638	Antiproliferative against human L-363 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human L-363 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
LN-229	EC₅₀	0.5 μM Compound: Chemical probe: UNC0638	Antiproliferative against human LN-229 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human LN-229 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
LNCaP	EC₅₀	0.3 μM Compound: Chemical probe: UNC0638	Antiproliferative against human LNCaP cells after 5 days by Cell-Titer Glo assay Antiproliferative against human LNCaP cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
MCF7	IC₅₀	0.07 μM Compound: 5, UNC0638	Inhibition of G9a in human MCF7 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human MCF7 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
MCF7	IC₅₀	6.99 μM Compound: UNC0638	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay	[PMID: 27720557]
MCF7	IC₅₀	81 nM Compound: 11, UNC0638	Inhibition of G9a in human MCF7 cells after 48 hrs by clonogenic assay Inhibition of G9a in human MCF7 cells after 48 hrs by clonogenic assay	[PMID: 22975593]
MDA-MB-231	EC₅₀	11 μM Compound: 126, UNC0638	Cytotoxicity against human MDA-MB-231 cells by MTT assay Cytotoxicity against human MDA-MB-231 cells by MTT assay	10.1039/C1MD00199J
MDA-MB-231	EC₅₀	11 μM Compound: 5, UNC0638	Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
MDA-MB-231	EC₅₀	11000 nM Compound: 4	Antiproliferative activity against human MDA-MB-231 cells by MTT assay Antiproliferative activity against human MDA-MB-231 cells by MTT assay	[PMID: 38799223]
MDA-MB-231	EC₅₀	11000 nM Compound: 5, UNC0638	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by Alamar Blue assay Cytotoxicity against human MDA-MB-231 cells after 48 hrs by Alamar Blue assay	[PMID: 24102134]
MDA-MB-231	IC₅₀	0.081 μM Compound: 5, UNC0638	Inhibition of G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
MDA-MB-231	IC₅₀	3.56 μM Compound: 47; UNC0638	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 35525212]
MDA-MB-231	IC₅₀	81 nM Compound: 11, UNC0638	Inhibition of G9a in human MDA-MB-231 cells after 48 hrs by clonogenic assay Inhibition of G9a in human MDA-MB-231 cells after 48 hrs by clonogenic assay	[PMID: 22975593]
MDA-MB-231	IC₅₀	81 nM Compound: 126, UNC0638	Inhibition of G9a/GLP in human MDA-MB-231 cells assessed as reduction of H3K9me2 level after 48 hrs by flow cytometric analysis Inhibition of G9a/GLP in human MDA-MB-231 cells assessed as reduction of H3K9me2 level after 48 hrs by flow cytometric analysis	10.1039/C1MD00199J
MDA-MB-231	IC₅₀	81 nM Compound: 38; UNC0638	Reduction in H3K9me2 level in human MDA-MB-231 cells incubated for 48 hrs by ChIP assay Reduction in H3K9me2 level in human MDA-MB-231 cells incubated for 48 hrs by ChIP assay	[PMID: 36528996]
MDA-MB-231	IC₅₀	81 nM Compound: 4	Downregulation of H3K9me2 level in human MDA-MB-231 cells measured after 48 hrs by Western blot analysis Downregulation of H3K9me2 level in human MDA-MB-231 cells measured after 48 hrs by Western blot analysis	[PMID: 38799223]
MDA-MB-231	IC₅₀	81 nM Compound: 5, UNC0638	Inhibition of lysine methyltransferase G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay Inhibition of lysine methyltransferase G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay	[PMID: 24102134]
MOLT-16	EC₅₀	0.2 μM Compound: Chemical probe: UNC0638	Antiproliferative against human MOLT-16 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human MOLT-16 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
MOLT-4	GI₅₀	188 nM Compound: 5; UNC0638	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth with replenishment of medium with compound on day 4 and 7 and measured after 12 days by ATPlite assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth with replenishment of medium with compound on day 4 and 7 and measured after 12 days by ATPlite assay	[PMID: 36882960]
MOLT-4	GI₅₀	188 nM Compound: 5; UNC0638	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth with replenishment of medium with compound on day 4 and 7 by ATPlite assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth with replenishment of medium with compound on day 4 and 7 by ATPlite assay	[PMID: 36882960]
MV4-11	EC₅₀	1.7 μM Compound: Chemical probe: UNC0638	Antiproliferative against human MV4-11 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human MV4-11 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H1975	EC₅₀	> 10 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H1975 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H1975 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H2009	EC₅₀	3.9 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H2009 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H2009 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H358	EC₅₀	4.3 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H358 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H358 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H441	EC₅₀	8.7 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H441 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H441 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H522	EC₅₀	1.5 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H522 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H522 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H661	EC₅₀	4.9 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H661 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H661 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H929	EC₅₀	4.6 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H929 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H929 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
OPM-2	EC₅₀	5.6 μM Compound: Chemical probe: UNC0638	Antiproliferative against human OPM-2 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human OPM-2 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
PA-1	EC₅₀	0.2 μM Compound: Chemical probe: UNC0638	Antiproliferative against human PA-1 cells after 7 days by Cell-Titer Glo assay Antiproliferative against human PA-1 cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
PC-3	EC₅₀	14 μM Compound: 5, UNC0638	Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
PC-3	IC₅₀	0.059 μM Compound: 5, UNC0638	Inhibition of G9a in human PC3 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human PC3 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
RD	CC₅₀	34.2 μM Compound: UNC-0638	Cytotoxicity against human RD cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human RD cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37021456]
RD	IC₅₀	11.17 μM Compound: 47; UNC0638	Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 24 hrs Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 24 hrs	[PMID: 35525212]
RD	IC₅₀	2.91 μM Compound: 47; UNC0638	Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 144 hrs Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 144 hrs	[PMID: 35525212]
RD	IC₅₀	3.05 μM Compound: 47; UNC0638	Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 35525212]
RPMI-8226	EC₅₀	5.1 μM Compound: Chemical probe: UNC0638	Antiproliferative against human RPMI-8226 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human RPMI-8226 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
RS4-11	EC₅₀	3.1 μM Compound: Chemical probe: UNC0638	Antiproliferative against human RS4-11 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human RS4-11 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
SJRH30	IC₅₀	2.48 μM Compound: 47; UNC0638	Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 144 hrs Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 144 hrs	[PMID: 35525212]
SJRH30	IC₅₀	2.64 μM Compound: 47; UNC0638	Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 35525212]
SJRH30	IC₅₀	5.01 μM Compound: 47; UNC0638	Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 24 hrs Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 24 hrs	[PMID: 35525212]
SK-BR-3	EC₅₀	0.6 μM Compound: Chemical probe: UNC0638	Antiproliferative against human SK-BR-3 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human SK-BR-3 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
SK-N-MC	EC₅₀	0.2 μM Compound: Chemical probe: UNC0638	Antiproliferative against human SK-N-MC cells after 7 days by Cell-Titer Glo assay Antiproliferative against human SK-N-MC cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
SW982	CC₅₀	29.46 μM Compound: UNC-0638	Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37021456]
Sf9	IC₅₀	13 nM Compound: UNC0638	Inhibition of N-terminal GST tagged human recombinant EHMT1 (794 to 1294 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay Inhibition of N-terminal GST tagged human recombinant EHMT1 (794 to 1294 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay	[PMID: 31350126]
Sf9	IC₅₀	26 nM Compound: UNC0638	Inhibition of N-terminal GST tagged human recombinant EHMT2 (785 to 1210 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay Inhibition of N-terminal GST tagged human recombinant EHMT2 (785 to 1210 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay	[PMID: 31350126]
THP-1	EC₅₀	4.9 μM Compound: Chemical probe: UNC0638	Antiproliferative against human THP-1 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human THP-1 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
THP-1	IC₅₀	0.24 μM Compound: 47; UNC0638	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 144 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 144 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 35525212]
THP-1	IC₅₀	0.34 μM Compound: 47; UNC0638	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 35525212]
THP-1	IC₅₀	0.84 μM Compound: 47; UNC0638	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 35525212]
U-937	IC₅₀	19.72 μM Compound: Chemical Probe: UNC0638	Cytotoxicity against human U-937 cells assessed as decrease in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human U-937 cells assessed as decrease in cell viability measured after 48 hrs by MTT assay	[PMID: 25978433]
U-937	IC₅₀	21.4 μM Compound: Chemical Probe: UNC0638	Cytotoxicity against human U-937 cells assessed as decrease in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human U-937 cells assessed as decrease in cell viability measured after 24 hrs by MTT assay	[PMID: 25978433]
U2OS	EC₅₀	0.5 μM Compound: Chemical probe: UNC0638	Antiproliferative against human U2OS cells after 7 days by Cell-Titer Glo assay Antiproliferative against human U2OS cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
ZR-75-30	EC₅₀	1.2 μM Compound: Chemical probe: UNC0638	Antiproliferative against human ZR-75-30 cells after 7 days by Cell-Titer Glo assay Antiproliferative against human ZR-75-30 cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]

体外研究
(In Vitro)

UNC0638 是 G9a 和 GLP 的抑制剂，对多种表观遗传和非表观遗传靶点具有优异的药效和选择性。UNC0638 的 K_i 测定值为 3.0 nM。UNC0638 的 Morrison K_i 为 3.7 nM。评估了 UNC0638 对多种表观遗传靶点的选择性。值得注意的是，UNC0638 对其他 H3K9 (SUV39H1 和 SUV39H2)、H3K27 (EZH2)、H3K4 (SETD7、MLL 和 SMYD3)、H3K79 (DOT1L) 和 H4K20 (SETD8) 甲基转移酶以及 PRDM1、PRDM10 和 PRDM12 无活性。此外，UNC0638 对蛋白质精氨酸甲基转移酶 PRMT1 和 PRMT3 以及组蛋白乙酰转移酶 HTATIP 无活性。值得注意的是，UNC0638 对 JMJD2E (IC₅₀=4,500 nM)、Jumonji 蛋白质去甲基化酶和 DNA 甲基转移酶 DNMT1 (IC₅₀=107,000 nM)具有较弱但可测量的活性。尽管如此，UNC0638 对 G9a 和 GLP 的选择性是 JMJD2E 的 200 倍以上，对 G9a 和 GLP 的选择性是 DNMT1 的 5,000 倍以上^[1]。
UNC0638 是一类能够特异性抑制组蛋白甲基转移酶 EHMT 的酶活性，降低细胞内 H3K9 二甲基化 (H3K9me2) 水平的小分子^[2]。

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

分子量

509.73

Formula

C₃₀H₄₇N₅O₂

CAS 号

1255580-76-7

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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

1M HCl 中的溶解度 : 100 mg/mL (196.18 mM; 超声助溶; 酸性条件溶解 (HCl 调节，pH≈1))

DMSO 中的溶解度 : 33.33 mg/mL (65.39 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9618 mL	9.8091 mL	19.6182 mL
5 mM	0.3924 mL	1.9618 mL	3.9236 mL
10 mM	0.1962 mL	0.9809 mL	1.9618 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

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 (4.90 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 (4.90 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 (4.90 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。

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: 99.48%

选择批次：

Data Sheet (646 KB) SDS (392 KB)

COA (286 KB) HNMR (292 KB) RP-HPLC (246 KB) LCMS (95 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Vedadi M, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74. [Content Brief]

[2]. Fu L, et al. Effects of the Histone Methyltransferase Inhibitor UNC0638 on Histone H3K9 Dimethylation of Cultured Ovine Somatic Cells and Development of Resulting Early Cloned Embryos. Reprod Domest Anim. 2014 Apr;49(2):e21-5. [Content Brief]

[3]. Singh N, et al. Inhibition of EHMT2 Induces a Robust Antiviral Response Against Foot-and-Mouth Disease and Vesicular Stomatitis Virus Infections in Bovine Cells. J Interferon Cytokine Res. 2016 Jan;36(1):37-47. [Content Brief]

[4]. Nualkaew T, et al. UNC0638 induces high levels of fetal hemoglobin expression in β-thalassemia/HbE erythroid progenitor cells[J]. Annals of hematology, 2020, 99: 2027-2036. [Content Brief]

Cell Assay	MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration	MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Vedadi M, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74. [Content Brief] [2]. Fu L, et al. Effects of the Histone Methyltransferase Inhibitor UNC0638 on Histone H3K9 Dimethylation of Cultured Ovine Somatic Cells and Development of Resulting Early Cloned Embryos. Reprod Domest Anim. 2014 Apr;49(2):e21-5. [Content Brief] [3]. Singh N, et al. Inhibition of EHMT2 Induces a Robust Antiviral Response Against Foot-and-Mouth Disease and Vesicular Stomatitis Virus Infections in Bovine Cells. J Interferon Cytokine Res. 2016 Jan;36(1):37-47. [Content Brief] [4]. Nualkaew T, et al. UNC0638 induces high levels of fetal hemoglobin expression in β-thalassemia/HbE erythroid progenitor cells[J]. Annals of hematology, 2020, 99: 2027-2036. [Content Brief]

UNC0638 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 / 1M HCl	1 mM	1.9618 mL	9.8091 mL	19.6182 mL	49.0456 mL
	5 mM	0.3924 mL	1.9618 mL	3.9236 mL	9.8091 mL
	10 mM	0.1962 mL	0.9809 mL	1.9618 mL	4.9046 mL
	15 mM	0.1308 mL	0.6539 mL	1.3079 mL	3.2697 mL
	20 mM	0.0981 mL	0.4905 mL	0.9809 mL	2.4523 mL
	25 mM	0.0785 mL	0.3924 mL	0.7847 mL	1.9618 mL
	30 mM	0.0654 mL	0.3270 mL	0.6539 mL	1.6349 mL
	40 mM	0.0490 mL	0.2452 mL	0.4905 mL	1.2261 mL
	50 mM	0.0392 mL	0.1962 mL	0.3924 mL	0.9809 mL
	60 mM	0.0327 mL	0.1635 mL	0.3270 mL	0.8174 mL
1M HCl	80 mM	0.0245 mL	0.1226 mL	0.2452 mL	0.6131 mL
1M HCl	100 mM	0.0196 mL	0.0981 mL	0.1962 mL	0.4905 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.

Keywords:

UNC06381255580-76-7UNC 0638UNC-0638VSVHistone MethyltransferaseAutophagyInfluenza VirusVesicular Stomatitis VirusInhibitorinhibitorinhibit

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