KYA1797K, Wnt/β-catenin Inhibitor

KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 ~0.75 µM (TOPflash assay). It binds directly to the regulators of G-protein signaling domain of axin, initiating β-catenin and Ras degradation through enhancement of the β-catenin destruction complex activating GSK3β. KYA1797K can effectively suppress the growth of CRCs harboring APC and KRAS mutations, as shown by various in vitro studies and by in vivo studies using xenograft and transgenic mouse models of tumors induced by APC and KRAS mutations. Destabilization of both β-catenin and Ras via targeting axin is a potential therapeutic strategy for treatment of CRC and other type cancers activated Wnt/β-catenin and Ras pathways.

Product information

CAS Number: 1956356-56-1

Molecular Weight: 442.51

Formula: C17H11KN2O6S2

Chemical Name: potassium (Z)-3-(5-((5-(4-nitrophenyl)furan-2-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)propanoate

Smiles: [K+].[O-]C(=O)CCN1C(=O)/C(=C/C2=CC=C(O2)C2C=CC(=CC=2)[N+]([O-])=O)/SC1=S

InChiKey: PHUNRLYHXGMOLG-WQRRWHLMSA-M

InChi: InChI=1S/C17H12N2O6S2.K/c20-15(21)7-8-18-16(22)14(27-17(18)26)9-12-5-6-13(25-12)10-1-3-11(4-2-10)19(23)24;/h1-6,9H,7-8H2,(H,20,21);/q;+1/p-1/b14-9-;

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO up to 100 mM

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:

KYA1797K was suggested to be used at 25 µM final concentration in vitro.

In Vivo:

KYA1797K was used to dose mice at 20-25 mg/kg by intraperitoneal injection in xenograft model of D-MT cell line that harbors both APC and KRAS mutations, or in Apcmin/+/KrasG12D LA2 mouse model.

References:

1. Cha PH, et al.Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation. (2016) Nat Chem Biol. 12(8):593-600.

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

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