SSTC3

Research use only, not for human use.

SSTC3 is a novel small-molecule CK1α activator with EC50 of 30 nM (WNT-driven reporter gene assay), Kd of 32 nM.

SSTC3 is a novel small-molecule CK1α activator with EC50 of 30 nM (WNT-driven reporter gene assay), Kd of 32 nM; has better pharmacokinetic properties than pyrvinium, attenuates the growth of such Apc mutant organoids with EC50 of 2.9 uM; 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; also attenuates the growth of patient-derived metastatic CRC xenograft, with minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.

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.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.

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. Animal Model:Five-week-old Apcmin 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.

SSTC 3 | SSTC-3

Metabolic Enzyme/Protease

Casein Kinase

Casein Kinase

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1242422-09-8

518.529

C23H17F3N4O3S2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (241.07 mM)

CN(C1=CC=C(C=C1)C(F)(F)F)S(=O)(=O)C2=CC=C(C=C2)C(=O)NC3=NC(=CS3)C4=CC=CC=N4

4-(N-methyl-N-(4-(trifluoromethyl)phenyl)sulfamoyl)-N-(4-(pyridin-2-yl)thiazol-2-yl)benzamide

(-20℃)

With Ice Pack

≥ 2 years