MC180295

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MC180295 (MC-180295, MC 180295) 是一种新型强效、高选择性 CDK9 抑制剂，IC50 为 5 nM

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; also shows high selectivity against a panel of 250 kinases at 1 uM; 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; demonstrates broad anti-cancer activity in vitro and is effective in in vivo cancer models; also sensitize 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.

MC180295 is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs, such as CDK1-Cyclin B (IC50, 138 nM), CDK2-Cyclin A (IC50, 233 nM), CDK2-Cyclin E (IC50, 367 nM), CDK3-Cyclin E (IC50, 399 nM), CDK4-Cyclin D (IC50, 112 nM), CDK5-P35 (IC50, 159 nM), CDK5-P25 (IC50, 186 nM), CDK6-Cyclin D3 (IC50, 712 nM), and CDK7-CycH/MAT1 (IC50, 555 nM). MC180295 also inhibits GSK-3α and GSK-3β.MC180295 (500 nM) reactivates epigenetically silenced genes by targeting CDK9 without affecting DNA methylation.MC180295 (0.1 μM) inhibits the proliferation in cancer cells.

MC180295 (20 mg/kg, i.p., qod) inhibits significant anti-tumor activity in mice bearing SW48 cells, shows no inhibitory activity against human T cell growth in vivo.

MC-180295 | MC 180295

Angiogenesis

CDK

CDK

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2237942-08-2

358.416

C17H18N4O3S

>98% (HPLC)

DMSO : 100 mg/mL 279.01 mM

O=C(C1=C(N)N=C(N[C@@H]2C(C3)CCC3C2)S1)C4=CC=CC=C4[N+]([O-])=O

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

(-20℃)

With Ice Pack

≥ 2 years