|2-环己基-N-(1-异丙基哌啶-4-基)-6-甲氧基-7-(3-(吡咯烷-1-基)丙氧基)喹唑啉-4-胺|CsnPharm

CAS No.: 1255580-76-7

UNC0638 Catalog No. CSN16350

Synonyms: UNC0638

UNC0638 is an inhibitor of protein lysine methyltransferases G9a and GLP with IC50 of < 15 nM, 19 nM, respectively.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述UNC0638 is a G9a/GLP inhibitor with IC50 value of 12nM in a SAHH-coupled assay and reduced cellular H3K9me2 with IC50 value of 81nM in cell western assay. It exhibited cytotoxicity with EC50 value up to 11μM in MDA-MB-231 cells, a large toxicity/function ratio of 140. It effectively inhibited the demethylation of p53 K373 in H1299 cells at concentration of 0.25μM post 24h. UNC0638 markedly reduced the clonogenicity of MCF7 cells, reduced the abundance of H3K9me2 marks at promoters of known G9a-regulated endogenous genes and disproportionately affected several genomic loci encoding microRNAs. It reactivated G9a-silenced genes and a retroviral reporter gene in a concentration-dependent manner without promoting differentiation in mouse embryonic stem cells.
作用机制UNC0638 is a substrate-competitive inhibitor, but does not compete with the cofactor SAM, which is distinguished with the other inhibitor. ^[2]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
22Rv1 cells	-	Function assay	-	Inhibition of G9a in human 22Rv1 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay, IC50=0.048 μM	21780790
H1299 cells	0.25 uM	Function assay	24 h	Inhibition of G9a expressed in H1299 cells assessed as inhibition of dimethylation of p53 at lys 373 at 0.25 uM after 24 hrs by Western blot analysis	21780790
HCT116 cells	-	Function assay	-	Inhibition of G9a in human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay, IC50=0.21 μM	21780790

更多
动物研究
剂量
Mice: 5 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 5 mg/kg^[3] (i.p.)
给药途径	i.p.

[1] Liu F, Barsyte-Lovejoy D, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50.
[2] Vedadi M, Barsyte-Lovejoy D, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9618 mL
- 9.8092 mL
- 19.6184 mL
- 5 mM
- 0.3924 mL
- 1.9618 mL
- 3.9237 mL
- 10 mM
- 0.1962 mL
- 0.9809 mL
- 1.9618 mL

技术信息

CAS号

1255580-76-7

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H47N5O2

运输

蓝冰

分子量

509.73

别名

UNC0638

溶解度

DMSO	50.0 mg/mL (98.1 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

UNC0638 Catalog No. CSN16350

靶点选择性

请登录您的专属账户

确认信息