For research use only. Not for therapeutic Use.
KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.
KYA1797K 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 GSK3b. KYA1797K effectively suppresses the growth of CRCs harboring APC and KRAS mutations. KYA1797K enhances formation of the β-catenin destruction complex and induced GSK3β activation, leading to phosphorylation of both β-catenin and K-Ras at S33/S37/T41 and T144/T148. KYA1797K degrades both β-catenin and Ras SW480, LoVo, DLD1 and HCT15 cells in a dose-dependent manner. KYA1797K destabilizes β-catenin and Ras in DLD1 cells expressing WT β-catenin or WT K-Ras[1].
KYA1797K significantly suppresses tumor growth and progression both in mouse xenografts of CRC cells harboring APC and K-Ras mutations and in an Apcmin/+/KRASG12DLA2 mouse model. KYA1797K administration (25 mg/kg) reduces both weight and volume of the tumor by 70%. KYA1797K treatment significantly reduces levels of β-catenin and Ras proteins as well as Wnt/β-catenin and Ras signaling targets [1].
| Catalog Number | I011941 |
| CAS Number | 1956356-56-1 |
| Synonyms | potassium;3-[(5Z)-5-[[5-(4-nitrophenyl)furan-2-yl]methylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]propanoate |
| Molecular Formula | C17H11KN2O6S2 |
| Purity | ≥95% |
| 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-; |
| InChIKey | PHUNRLYHXGMOLG-WQRRWHLMSA-M |
| SMILES | C1=CC(=CC=C1C2=CC=C(O2)C=C3C(=O)N(C(=S)S3)CCC(=O)[O-])[N+](=O)[O-].[K+] |
| Reference | [1]. Cha PH, et al. Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation. Nat Chem Biol. 2016 Aug;12(8):593-600. |
