SY-5102

SY-5102 is a potent, selective and orally active cyclin-dependent kinase (CDK7) inhibitor with a K_d of 0.03 nM. SY-5102 shows anti-proliferative activity against HCC70 cells with an EC₅₀ of 9 nM. SY-5102 can inhibit CDK7-mediated CAK function (downregulate CDK2 Thr160 phosphorylation) and TFIIH transcription function (downregulate RNA polymerase II Ser5 phosphorylation). SY-5102 can induce G2/M cell cycle arrest, downregulate the expression of the oncogene c-Myc, and ultimately trigger cancer cell apoptosis. SY-5102 can be used for the research of triple-negative breast cancer (TNBC).

• Data Sheet (273 KB)