BS-181

BS-181 is a highly selective, small-molecule inhibitor of cyclin-dependent kinase 7 (CDK7) with an IC50 of 21 nM. Developed by researchers at Imperial College London in collaboration with Emory University and Cancer Research UK, BS-181 demonstrates over 40-fold selectivity for CDK7 compared to other CDKs, such as CDK1, CDK2, CDK4, CDK5, CDK6, and CDK9. By blocking CDK7, BS-181 inhibits the phosphorylation of RNA polymerase II and the estrogen receptor, leading to cell cycle arrest and apoptosis in various cancer cell lines, including breast, gastric, colorectal, and lung cancers. Due to poor oral bioavailability and pharmacokinetic properties, BS-181 was not advanced into clinical trials; however, it served as a foundational chemical probe that led to the development of the clinical-stage CDK7 inhibitor samuraciclib (ICEC0942).

Other names

BS 181BS181BS-181BS-181 dihydrochlorideBS181 dihydrochlorideBS 181 dihydrochloride