BS-181-L

BS-181-L is a selective, potent, and orally bioavailable small molecule inhibitor of cyclin-dependent kinase 7 (CDK7), developed by researchers at Imperial College London. It was designed as an optimized successor to BS-181, featuring improved pharmacokinetic properties, aqueous solubility, and oral bioavailability. CDK7 plays a dual role in regulating cell cycle progression (as part of the CDK-activating kinase complex) and transcription (by phosphorylating the C-terminal domain of RNA polymerase II). Preclinically, BS-181-L has demonstrated efficacy in inhibiting tumor cell growth in breast cancer (MCF7) and colorectal cancer (HCT116) models, downregulating key biomarkers, and reducing estrogen receptor activity, making it a promising candidate for breast cancer therapy.