RGB-286147 (RGB 286147) is a proteome-wide CDK/CRK-specific kinase inhibitor with IC50 of 48 and 15 nM for CDK1/CycB and CDK2/CycE, respectively.
RGB-286147 weakly inhibits CDK4/6 and GSK3b with IC50 of 839/282 and 754 nM, respectively.
RGB-286147 inhibited the kinase activity of CDK3, CDK5, and CDK7, with similar potency (low nanomolar IC50 values, 10-70 nM).
RGB-286147 also inhibited the autophosphorylation of CDK9 as well as the crossphosphorylation of cyclin T1 by CDK9 in a dose-dependent manner and with comparable potency.
RGB-286147 is a potential CDK20 inhibitor.
RGB-286147 caused a pronounced G1 arrest, endoreduplication, and apoptotic cell death in HCT116 cells, inhibited HCT116 cell viability with IC50 of 57 nM (24h).
RGB-286147 is a highly potent and broad-spectrum inhibitor of tumor cell growth with average GI50 of <10 nM at 48 hr of exposure.
