SSTC3 is a novel small-molecule CK1α activator with EC50 of 30 nM (WNT-driven reporter gene assay), Kd of 32 nM.
SSTC3 has better pharmacokinetic properties than pyrvinium (Cat# PC-60383), attenuates the growth of such Apc mutant organoids with EC50 of 2.9 uM.
SSTC3 decreases the viability of the WNT-dependent cell lines (EC50 = 132, 63, and 123 nM for HT29, SW403, and HCT116 cells, respectively), inhibits the growth of CRC xenografts in mice.
SSTC3 also attenuates the growth of patient-derived metastatic CRC xenograft, with minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
