KYA1797K is a potent and highly selective Wnt/β-catenin inhibitor with an IC50 of 0.75 μM in TOPflash experiments.

 

Brand: BCM

 

Target: Wnt/beta-catenin

 

Signaling Pathways: Cytoskeletal Signaling; Stem Cells

 

In Vitro: KYA1797K significantly decreases reporter activities for the Wnt/β-catenin and MAPK/ERK pathways but does not affect the reporter activities of other cancer-related pathways, such as the Notch and TGFβ pathways, thus, KYA1797K selectively regulates the Wnt/β-catenin and Ras/ERK pathways. KYA1797K enhances the β-catenin binding affinity of endogenous axin, GSK3β and β-TrCP. Interaction between APC and β-catenin is not enhanced by KYA1797K. It promotes the formation of the β-catenin destruction complex. KYA1797K degrades both β-catenin and Ras in these cells(CRC lines SW480, LoVo, DLD1 and HCT15) in a dose-dependent manner, cell proliferation is also suppressed by KYA1797K treatment. KYA1797K inhibits proliferation of CRC cells mainly via destabilization of β-catenin with additional Ras degradation. KYA1797K directly targeted axin and modulated conformation of the β-catenin destruction complex.

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

Isomeric SMILES: C1=CC(=CC=C1C2=CC=C(O2)/C=C\3/C(=O)N(C(=S)S3)CCC(=O)[O-])[N+](=O)[O-].[K+]  

 

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-; 

 

Attribute
[Chem Name]	potassium;3-[(5Z)-5-[[5-(4-nitrophenyl)furan-2-yl]methylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]propanoate
[Synonym]	KYA1797K
[CAS No.]	1956356-56-1
[MDL No.]	MFCD30718585
[Formula]	C17H11KN2O6S2
[Molecular]	442.50734
[Form]	A crystalline solid
[Storage]	Inert atmosphere, 2-8°C

Goods Tag