Chemical Structure : CDK inhibitor E9
Catalog No.: PC-63235Not For Human Use, Lab Use Only.
CDK inhibitor E9 is a novel CDK inhibitor that can overcomes ABC-mediated resistance of THZ1, functions as a potent, non-covalent inhibitor of CDK9 and a covalent inhibitor of CDK12.
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CDK inhibitor E9 is a novel CDK inhibitor that can overcomes ABC-mediated resistance of THZ1, functions as a potent, non-covalent inhibitor of CDK9 and a covalent inhibitor of CDK12; does not serve as a substrate for either ABCB1 or ABCG2, while avoiding ABC transporter-mediated efflux; decreases the phosphorylated and total RNAPII in THZ1R NB and lung cancer cells (IC50=8-40 nM), accompanied by decreased MYC and MCL1 expression, exerts its cytotoxic effects through covalent modification of cysteine 1039 of CDK12.
M.Wt | 434.544 | |
Formula | C24H30N6O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Gao Y, et al. Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5.
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