An inhibitor of Wnt/β-catenin signaling; inhibits expression of a reporter induced by Wnt3a-conditioned medium in HEK293 cells (IC50 = 0.75 μM); binds to the RGS domain of axin and increases activation of GSK3β

KYA1797K – 10 mg

Brand:
Cayman
CAS:
1956356-56-1
Storage:
-20
UN-No:
Non-Hazardous - /

KYA1797K is an inhibitor of Wnt/β-catenin signaling.{46795} 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.  

 

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SKU: 29221 - 10 mg Category:

Description

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

Formal name: (5Z)-5-[[5-(4-nitrophenyl)-2-furanyl]methylene]-4-oxo-2-thioxo-3-thiazolidinepropanoic acid, monopotassium salt

Synonyms: 

Molecular weight: 442.5

CAS: 1956356-56-1

Purity: ≥95%

Formulation: A crystalline solid

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