SR-3029

SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC₅₀s of 44 nM and 260 nM, respectively, and K_is of 97 nM for both kinases. IC50 & Target: IC50: 44 nM (CK1δ) and 260 nM (CK1ε)^[1]
Ki: 97 nM (CK1δ/CK1ε)^[1] In Vitro: SR-3029 is a potent CK1δ/CK1ε inhibitor, with IC₅₀s of 44 nM and 260 nM, respectively. SR-3029 is ATP competitive, with K_is of 97 nM for CK1δ/CK1ε. SR-3029 also blocks CDK6/cyclin D3, CDK6/cyclin D1, CDK4/cyclin D3, CDK4/cyclin D1 and FLT3, with IC₅₀s of 427, 428, 368, 576, and 3000 nM, respectively. SR-3029 shows inhibitory effects on A375 cells, with an EC₅₀ of 86 nM^[1]. CK1δ is a necessary and sufficient driver of Wnt/β-catenin signaling in human breast cancer. SR-3029 shows less potent activities against MCF7 and T47D breast cancer cells and the MCF10A cell line, which express low amounts of CK1δ^[2]. In Vivo: SR-3029 (20 mg/kg daily i.p.) exibits anti-tumor effects in rthotopic MDA-MB-231, MDA-MB-468 (TNBC), SKBR3 and BT474 (HER2+) tumor xenografts with no overt toxicity in mice. SR-3029 (20 mg/kg daily i.p.) also effectively inhibits the growth of tumor in primary patient-derived xenograft (PDX) models. In addition, SR-3029 (20 mg/kg, i.p.) strongly reduces the expression of nuclear β-catenin in tumors of mice^[2].