产品描述:
SR 3029 is an inhibitor of casein kinase 1δ (CK1δ) and CK1ε (IC50s = 44 and 260 nM, respectively).{47522} It is selective for CK1δ and CK1ε over 438 kinases in a panel but also inhibits MYLK4, FLT3, Cdk4/cyclin D1, and MARK2 by greater than 90% at 10 µM. SR 3029 inhibits Cdk4/cyclin D1, Cdk4/cyclin D3, Cdk6/cyclin D1, Cdk6/cyclin D3, and FLT3 with IC50 values of 576, 368, 428, 427, and 3,000 nM, respectively. It inhibits proliferation of A375 human melanoma cells in vitro (EC50 = 86 nM). SR 3029 (20 mg/kg per day) reduces tumor growth and increases lifespan in MDA-MB-231 and MDA-MB-468 mouse xenograft models.{47523} It reduces the expression of the Wnt/β-catenin target CCND1 and decreases protein levels of nuclear β-catenin and cyclin D1 in mouse tumor tissue.