ldc000067

Description: LDC000067 (also called LDC067) is a novel, potent, highly selective and ATP-competitive inhibitor of cyclin-dependent kinase (CDK9) with IC50 of 44 nM. CDK9 is an important therapeutic target but currently available inhibitors exhibit low specificity and/or narrow therapeutic windows. LDC000067 exhibited selectivity for CDK9 over other CDKs in the range of 55-fold (vs. CDK2) to over 230-fold (vs. CDK6 and CDK7). LDC067 also inhibited transcription in a dose-dependent and ATP-competitive manner. In whole cells, LDC000067 induced the tumor suppressor protein p53 activation and apoptosis. LDC000067 also selectively reduced short-lived mRNAs, including those that encode regulators of apoptosis and proliferation such as MYC and MCL1.

References: Br J Pharmacol. 2014 Jan; 171(1):55-68