Promotor of β-catenin and Ras degradation (IC50 value 0.75 μM for inhibition of TOPflash activity) that effectively suppresses the growth of CRCs (colorectal cancers) harboring APC and KRAS mutations in vitro and in vivo. KYA1797K binds the RGS domain of axin and enhances the binding affinity of β-catenin or Ras with the β-catenin destruction complex components, leading to simultaneous destabilization of β-catenin and Ras via GSK3β activation. KYA1797 also inhibits ASK1 (IC50 value 0.65 μM for inhibition of apoptosis signal-regulating kinase 1).

KEYWORDS: KYA1797K | supplier | dual ASK1 and Wnt/β-catenin inhibitor | KYA 1797K | CAS [1956356-56-1] | [ 851304-36-4] | Wnt Inhibitor | Axin | Axin1 | RGS domain | Ras | GSK3β activation | ASK1 | apoptosis signal-regulating kinase 1 | colorectal cancer | CRC | APC