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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-MC180295
MC180295

Chemical Structure : MC180295

CAS No.: 2237942-08-2

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MC180295 (MC-180295;MC 180295)

货号: PC-35808Not For Human Use, Lab Use Only.

MC180295 (MC-180295, MC 180295) is a novel potent, highly selective CDK9 inhibitor with IC50 of 5 nM, displays >22-fold selectivity over other CDKs.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MC180295 (MC-180295, MC 180295) is a novel potent, highly selective CDK9 inhibitor with IC50 of 5 nM, displays >22-fold selectivity over other CDKs.
MC180295 also shows high selectivity against a panel of 250 kinases at 1 uM.
MC180295 specificly inhibits the phosphorylation levels of Ser2 (pSer2); CDK9-mediated phosphorylation of BRG1 prevents it from being recruited to heterochromatin loci, while CDK9 inhibition allows BRG1 to remodel chromatin and alter gene expression.
MC180295 demonstrates broad anti-cancer activity in vitro and is effective in in vivo cancer models.
MC180295 also sensitizes to anti-PD1 in vivo, increases the numbers of CD45+ immune cells and the percentages of CD3+ T cells and activates dendritic cells in the tumor environment, while not kill human T lymphocytes and did not affect the ratio of CD4 and CD8 T cells in vivo.

物理化学性质&存储条件

分子量 358.416
分子式 C17H18N4O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

Rel-(4-amino-2-(((2S)-bicyclo[2.2.1]heptan-2-yl)amino)thiazol-5-yl)(2-nitrophenyl)methanone

参考文献

1. Zhang H, et al. Cell. 2018 Nov 15;175(5):1244-1258.e26.

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