LDC000067

LDC000067 is a highly selective, ATP-competitive small molecule inhibitor of cyclin-dependent kinase 9 (CDK9) with an IC50 of 44 nM. It was developed by the Lead Discovery Center in collaboration with the Max Planck Institute of Immunobiology and Epigenetics and the University of Muenster. CDK9, in complex with cyclin T1, forms the positive transcription elongation factor b (P-TEFb) complex, which phosphorylates the C-terminal domain of RNA polymerase II to promote transcriptional elongation. By inhibiting CDK9, LDC000067 blocks P-TEFb-dependent transcription, leading to the selective down-regulation of short-lived oncogenic and anti-apoptotic proteins such as MYC and MCL-1, and inducing apoptosis in cancer cells. It is widely used as a research tool to study CDK9 biology and has shown preclinical efficacy in models of cancer (such as chordoma, osteosarcoma, and endometrial cancer), inflammatory conditions (such as sepsis-associated encephalopathy and osteoarthritis), and viral infections (such as influenza and HIV-1 latency).

Other names

(3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methanesulfonamide3-[[6-(2-methoxyphenyl)-4-pyrimidinyl]amino]-benzenemethanesulfonamide