SSTC3 is a casein kinase 1α (CK1α) activator ( K d = 32 nM) that inhibits WNT signaling ( EC 50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
In Vitro
SSTC3 (0-1μM, 5 days) decreases the viability of HCT116 cells in an on-target manner. This capacity is significantly reduced when the mutant CTNNB1 allele driving its carcinogenic properties is deleted. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Colorectal cancer (CRC) cell lines. Concentration: 0-1 μM. Incubation Time: 5 days. Result: Decreased the viability. Western Blot AnalysisCell Line: SW403 cells. Concentration: 100 nM. Incubation Time: 15 min. Result: Increased β-catenin phosphate levels.
In Vivo
SSTC3 can be maintained for 24 hours after treatment . SSTC3 (25 mg/kg, ip once daily for 8-12 days) suppresses the growth of colorectal carcinoma in CD-1 mice . SSTC3 (10 mg/kg, ip once daily for 1 month) inhibits the growth of Apc mutation-driven tumors . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Five-week-old Apc min mice . Dosage: 10 mg/kg. Administration: IP for 1 month. Result: Inhibited the growth of Apc mutation-driven tumors. Animal Model: CD-1 mice. Dosage: 25 mg/kg. Administration: IP once daily for 8-12 days. Result: Inhibited the growth of HCT116 xenografts. Attenuated the growth of this metastatic CRC PDX and markedly reduced the cell density of residual cancer. Reduced the expression of WNT biomarkers in this CRC PDX.
