Chemical Name: (5Z)-5-[[5-(4-Nitrophenyl)-2-furanyl]methylene]-4-oxo-2-thioxo-3-thiazolidinepropanoic acid potassium salt
Biological ActivityKYA 1797K is a Wnt/β-catenin signaling inhibitor (IC50 = 0.75 μM). Increases binding affinity of β-catenin for axin, GSK-3β and β-TrCP. Promotes formation of the destruction complex, activation of GSK-3β and phosphorylation of β-catenin and K-Ras, leading to their degradation via the ubiquitin/proteasome system. Reduces levels of β-catenin and K-Ras and inhibits growth of colorectal cancer (CRC) cells in vitro and in mouse xenograft models.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation.
Cha et al.
A Ras destabilizer KYA1797K overcomes the resistance of EGFR tyrosine kinase inhibitor in KRAS-mutated non-small cell lung cancer.
Park et al.
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