KI-ARv-03

KI-ARv-03 is a potent and selective ATP-competitive CDK9 inhibitor with an IC50 of 0.15 μM (in the presence of 45 μM ATP), demonstrating over 130-fold selectivity for CDK9 over other CDKs (including CDK1-7) . It reduces AR-driven transcription and proliferation in prostate cancer cells and is applicable for research on leukemia, pancreatic cancer, alveolar rhabdomyosarcoma (ARMS), and castration-resistant prostate cancer (CRPC) . Additionally, KI-ARv-03 serves as a ligand for target protein for PROTAC and is used in the synthesis of PROTAC KI-CDK9d-32.