MC180295

Research use only, not for human use.

MC180295 (MC-180295, MC 180295) is a novel potent, highly selective CDK9 inhibitor with IC50 of 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.

MC-180295;MC 180295

Angiogenesis

CDK

CDK

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2237942-08-2

358.42

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