M435-1279 是 UBE2T 抑制剂。M435-1279 通过阻断 UBE2T 介导的 RACK1 降解来抑制 Wnt/β-catenin 信号通路的过度激活。
货号:ajcx35536
CAS:1359431-16-5
分子式:C18H17N3O5S2
分子量：419.47
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1[1].

M435-1279 (0, 2, 4, 8, 16, 31 μM; 48 h) significantly inhibits the growth of HGC27, AGS, and MKN45 cells[1].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[1].M435-1279 (31 nM to 500 μM) binds to UBE2T with a KD value of 50.5 μM[1].M435-1279 (11.88 μM; 48 h) inhibits the ubiquitination of RACK1 and the hyperactivation of the Wnt/β-catenin pathway[1].

M435-1279 (5 mg/kg/day; intratumor injection for 18 days) slows the tumor growth[1].M435-1279 induces higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors[1].

[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: Oncogene. 2021 Apr;40(14):2622-2623.