KI-ARv-03 is a potent and selective ATP-competitive inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC₅₀ of 0.15 μM in the presence of 45 μM ATP, with over 130-fold selectivity for CDK9 relative to other CDKs. This compound effectively reduces androgen receptor (AR)-driven transcription and cellular proliferation in prostate cancer models. KI-ARv-03 is applicable in the study of various malignancies, including leukemia, pancreatic cancer, alveolar rhabdomyosarcoma, and castration-resistant prostate cancer. Additionally, it serves as a ligand for PROTAC synthesis, specifically for generating PROTAC KI-CDK9d-32.
KI-ARv-03 is a potent and selective ATP-competitive inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC₅₀ of 0.15 μM in the presence of 45 μM ATP, with over 130-fold selectivity for CDK9 relative to other CDKs. This compound effectively reduces androgen receptor (AR)-driven transcription and cellular proliferation in prostate cancer models. KI-ARv-03 is applicable in the study of various malignancies, including leukemia, pancreatic cancer, alveolar rhabdomyosarcoma, and castration-resistant prostate cancer. Additionally, it serves as a ligand for PROTAC synthesis, specifically for generating PROTAC KI-CDK9d-32.
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