SKLB06489 is a potent, selective type I PRMTs inhibitor with IC50 of 64.55, 4.21, and 51.27 nM for PRMT1, PRMT6, and PRMT8 respectively.
SKLB06489 dose-dependently inhibits cell proliferation and colony formation with IC50 values in the low micromolar range in TNBC cell lines MDA-MB-231, Hs578T, and BT549.
SKLB06489 (40, 80 mg·kg-1·d-1, i.g. for 33 days) dose-dependently suppressed tumor growth in MDA-MB-231 subcutaneous xenograft models.
SKLB06489 inhibited TNBC proliferation by impairing DNA replication, compromising DNA damage repair, and ultimately inducing G0/G1-phase cell cycle arrest and apoptosis.
SKLB06489 (5, 10 μΜ) dose-dependently enhanced intracellular cholesterol efflux in MDA-MB-231 cells and Hs578T cells via upregulation of the ATP-binding cassette transporter A1 (ABCA1) and ATP-binding cassette transporter G1 (ABCG1), thereby disrupting cholesterol metabolic homeostasis.