tcsc3391 LDC000067

LDC000067 is a highly specific CDK9 inhibitor with an IC₅₀ value of 44±10 nM in vitro.



IC50 & Target: IC50: 44±10 nM (CDK9-Cyclin T1), 2441 nM (CDK2-Cyclin A)^[1]

In Vitro: The selectivity of LDC000067 for CDK9 over other CDKs exceeds that of the known inhibitors flavopiridol and DRB. LDC000067 displayed 55/125/210/ >227/ >227-fold selectivity for CDK9 versus CDK2/1/4/6/7. LDC000067 inhibits in vitro transcription in an ATP-competitive and dose-dependent manner. Gene expression profiling of cells treated with LDC000067 demonstrates a selective reduction of short-lived mRNAs, including important regulators of proliferation and apoptosis^[1].