An inhibitor of Wnt/β-catenin signaling
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KYA1797K

Item No. 29221

Technical Information
Formal Name
(5Z)-5-[[5-(4-nitrophenyl)-2-furanyl]methylene]-4-oxo-2-thioxo-3-thiazolidinepropanoic acid, monopotassium salt
CAS Number
1956356-56-1
Molecular Formula
C17H11N2O6S2 • K
Formula Weight
Purity
≥95%
A crystalline solid
DMF: Partially solubleDMSO: 0.5 mg/mlEthanol: Partially solublePBS (pH 7.2): 0.3 mg/ml
λmax
240, 327, 436 nm
SMILES
O=C(N(CCC([O-])=O)C(S/1)=S)C1=C\C2=CC=C(C3=CC=C([N+]([O-])=O)C=C3)O2.[K+]
InChi Code
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-;
InChi Key
PHUNRLYHXGMOLG-WQRRWHLMSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    KYA1797K is an inhibitor of Wnt/β-catenin signaling.1 It inhibits expression of a reporter induced by Wnt3a-conditioned medium in HEK293 cells (IC50 = 0.75 μM). KYA1797K binds to the regulators of G-protein signaling (RGS) domain of axin and increases activation of GSK3β, as well as phosphorylation of β-catenin and Ras, in HEK293 cells when used at a concentration of 25 μM. It decreases β-catenin and Ras protein levels and inhibits colony formation in SW480 cells in a concentration-dependent manner. KYA1797K inhibits the growth of SW480, LoVo, DLD1, and HCT15 cells (GI50s = 5, 4.8, 4.5, and 4.2 μM, respectively). It reduces tumor growth in a D-MT colorectal cancer mouse xenograft model when administered at a dose of 20 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cha, P.-H., Cho, Y.-H., Lee, S.-K., et alSmall-molecule binding of the axin RGS domain promotes β-catenin and ras degradation. Nat. Chem. Biol. 12(8), 593-600 (2016).