Description
SSTC3 is a novel small-molecule CK1alpha activator with EC50 of 30nM (WNT-driven reporter gene assay), Kd of 32nM; has better pharmacokinetic properties than pyrvinium, attenuates the growth of such Apc mutant organoids with EC50 of 2.9uM; decreases the viability of the WNT-dependent cell lines (EC50=132, 63, and 123nM for HT29, SW403, and HCT116 cells, respectively), inhibits the growth of CRC xenografts in mice; also attenuates the growth of patient-derived metastatic CRC xenograft, with minimal gastrointestinal toxicity compared to other classes of WNT inhibitors