KYA1797K - Wnt 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEKYA1797KCat. No.: HY-101090CAS No.: 1956356-56-1分式: CHKNOS分量: 442.51作靶點(diǎn): Wnt; -catenin作通路: Stem Cell/Wnt儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 6 mg/mL (13.56 mM; Need ultrasonic)H2

2、O : 1 mg/mL (2.26 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.2598 mL 11.2992 mL 22.5984 mL5 mM 0.4520 mL 2.2598 mL 4.5197 mL10 mM 0.2260 mL 1.1299 mL 2.2598 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 KYA1797K是有效，選擇性的 Wnt/-catenin 抑制劑，IC50 值為0.7

3、5 M。IC50 & Target IC50: 0.75 (Wnt/-catenin) 1體外研究KYA1797K binds directly to the regulators of G-protein signaling domain of axin, initiating b-catenin and Rasdegradation through enhancement of the b-catenin destruction complex activating GSK3b. KYA1797K1/2 Master of Small Molecules 您邊的抑制劑師www.MedChe

4、mEeffectively suppresses the growth of CRCs harboring APC and KRAS mutations. KYA1797K enhancesformation of the -catenin destruction complex and induced GSK3 activation, leading to phosphorylation ofboth -catenin and K-Ras at S33/S37/T41 and T144/T148. KYA1797K degrades both -catenin and RasSW480, L

5、oVo, DLD1 and HCT15 cells in a dose-dependent manner. KYA1797K destabilizes -catenin andRas in DLD1 cells expressing WT -catenin or WT K-Ras 1.體內(nèi)研究 KYA1797K significantly suppresses tumor growth and progression both in mouse xenografts of CRC cellsharboring APC and K-Ras mutations and in an Apcmin/+

6、/KrasG12DLA2 mouse model. KYA1797Kadministration (25 mg/kg) reduces both weight and volume of the tumor by 70%. KYA1797K treatmentsignificantly reduces levels of -catenin and Ras proteins as well as Wnt/-catenin and Ras signaling target1.PROTOCOLCell Assay 1 SW480, LoVo, DLD1 and HCT15 cells are tre

7、ated with KYA1797K (0.2, 1, 5, 25 M) for 24 h or 4 d. MTTassay is used to determine effects of KYA1797K on cell proliferation 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: KYA1797K (20 mg/kg) is injected intraperitoneally (i.p.) into mi

8、ce carrying xenografted tumors from theAdministration 1 D-MT cell line that harbors both APC and KRAS mutations for 28 days. Tumor weight is measured at time ofsacrifice and tumor volumes of mice are measured every 4 d 1.MCE has not independently confirmed the accuracy of these methods. They are for

9、 reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Cell Sci. 2019 Apr 26. pii: jcs.228478. Biochem Biophys Res Commun. 2018 Oct 12;504(4):941-948.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Cha PH, et al. Small-molecule binding of the axin RGS domain promotes -catenin and Ras degradation. Nat Chem Biol. 2016Aug;12(8):593-600.McePdfHeightCaution: Product has not been fully validated for med