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Biological Activity for KYA 1797K
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 for KYA 1797K
|Storage||Store at -20°C|
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.
Solubility Data for KYA 1797K
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||2.21||5 with gentle warming|
Preparing Stock Solutions for KYA 1797K
The following data is based on the product molecular weight 442.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.05 mM||45.2 mL||225.99 mL||451.98 mL|
|0.25 mM||9.04 mL||45.2 mL||90.4 mL|
|0.5 mM||4.52 mL||22.6 mL||45.2 mL|
|2.5 mM||0.9 mL||4.52 mL||9.04 mL|
References for KYA 1797K
References are publications that support the biological activity of the product.
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
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