M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.
性状
Solid
IC50 & Target[1][2]
UBE2T
体外研究(In Vitro)
M435-1279 (0, 2, 4, 8, 16, 31 μM; 48?h) significantly inhibits the growth of HGC27, AGS, and MKN45 cells.M435-1279 (0, 4, 8, 12, 16, 20 μM) inhibits the cell viability with IC50s of 16.8, 11.88, 6.93, 7.76 μM of GES-1, HGC27, MKN45, AGS cells, respectively.M435-1279 (31?nM to 500?μM) binds to UBE2T with a KD value of 50.5?μM.M435-1279 (11.88?μM; 48?h) inhibits the ubiquitination of RACK1 and the hyperactivation of the Wnt/β-catenin pathway. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
M435-1279 (5?mg/kg/day; intratumor injection for 18 days) slows the tumor growth.
M435-1279 induces higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Yu Z, et al. A novel UBE2T inhibitor suppresses Wnt/β-catenin signaling hyperactivation and gastric cancer progression by blocking RACK1 ubiquitination. Oncogene. 2021 Feb;40(5):1027-1042. doi: 10.1038/s41388-020-01572-w. Epub 2020 Dec 15. Erratum in: Onc
溶解度数据
In Vitro: DMSO : 50 mg/mL (119.20 mM; Need ultrasonic)配制储备液