SY-5102

SY-5102 is a potent, selective, orally active cyclin-dependent kinase (CDK7) inhibitor with a Kd of 0.03 nM. It exhibits antiproliferative activity against HCC70 cells with an EC50 of 9 nM. SY-5102 inhibits CDK7-mediated CAK function [downregulating CDK2Thr160 phosphorylation] and TFIIH transcription function [downregulating RNA polymerase II Ser5 phosphorylation]. The compound induces G2/M cell cycle arrest, downregulates the expression of the oncogene c-Myc, and ultimately triggers apoptosis in cancer cells. SY-5102 is applicable for research in triple-negative breast cancer (TNBC) .