KYA 1797K

Biological Activity

KYA 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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation.
   Cha et al.
   Nat.Chem.Biol., 2016;12:593
2. A Ras destabilizer KYA1797K overcomes the resistance of EGFR tyrosine kinase inhibitor in KRAS-mutated non-small cell lung cancer.
   Park et al.
   Sci.Rep., 2019;9:648

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