MC180295

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.