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Chemical Structure : MC180295
CAS No.: 2237942-08-2
Catalog No.: 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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|---|---|---|---|
| 5 mg | $188 | In stock | |
| 10 mg | $298 | In stock | |
| 25 mg | $498 | In stock | |
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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.
| M.Wt | 358.416 | |
| Formula | C17H18N4O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Rel-(4-amino-2-(((2S)-bicyclo[2.2.1]heptan-2-yl)amino)thiazol-5-yl)(2-nitrophenyl)methanone |
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1. Zhang H, et al. Cell. 2018 Nov 15;175(5):1244-1258.e26.
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