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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.
分子量 | 442.5 |
公式 | C17H11KN2O6S2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1956356-56-1 |
PubChem ID | 119057297 |
InChI Key | PHUNRLYHXGMOLG-WQRRWHLMSA-M |
Smiles | C1=CC(=CC=C1C2=CC=C(O2)/C=C\3/C(=O)N(C(=S)S3)CCC(=O)[O-])[N+](=O)[O-].[K+] |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Cha et al (2016) Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation. Nat.Chem.Biol. 12 593 PMID: 27294323
Park et al (2019) A Ras destabilizer KYA1797K overcomes the resistance of EGFR tyrosine kinase inhibitor in KRAS-mutated non-small cell lung cancer. Sci.Rep. 9 648 PMID: 30679620
关键词: KYA 1797K, KYA 1797K supplier, KYA1797K, wnt, beta, catenin, β, signaling, pathway, inhibitors, inhibits, K-Ras, destruction, complex, promotes, Beta-catenin, 7002, Tocris Bioscience
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