SKLB06489 is a selective and orally active type I PRMT enzyme inhibitor, with IC50 values of 64.55 nM for PRMT1, 4.21 nM for PRMT6, and 51.27 nM for PRMT8. It impedes cancer cell proliferation, colony formation, DNA replication, and DNA damage repair. SKLB06489 induces G0/G1 phase cell cycle arrest and apoptosis (apoptosis) in cancer cells. It disrupts cholesterol metabolic homeostasis by upregulating ABCA1 and ABCG1, promoting intracellular cholesterol efflux, and inhibiting tumor growth in subcutaneous xenograft models. SKLB06489 is useful for studying triple-negative breast cancer (TNBC).

PRMT1:64.55 nM