SSTC3

SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.

Product information

CAS Number: 1242422-09-8

Molecular Weight: 518.53

Formula: C23H17F3N4O3S2

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

Smiles: CN(C1C=CC(=CC=1)C(F)(F)F)S(=O)(=O)C1C=CC(=CC=1)C(=O)NC1=NC(=CS1)C1=CC=CC=N1

InChiKey: HSFAATUFWDDUGW-UHFFFAOYSA-N

InChi: InChI=1S/C23H17F3N4O3S2/c1-30(17-9-7-16(8-10-17)23(24,25)26)35(32,33)18-11-5-15(6-12-18)21(31)29-22-28-20(14-34-22)19-4-2-3-13-27-19/h2-14H,1H3,(H,28,29,31)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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.

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.

References:

1. Li B, Orton D, Neitzel LR, et al. Differential abundance of CK1α provides selectivity for pharmacological CK1α activators to target WNT-dependent tumors. Sci Signal. 2017;10(485):eaak9916. Published 2017 Jun 27. doi:10.1126/scisignal.aak9916

Products are for research use only. Not for human use.