M435-1279

M435-1279CAS号: 1359431-16-5分子式: C18H17N3O5S2分子量: 419.48描述纯度储存/保存方法可溶性/溶解性In vitro(体外研究)In vivo(体内研究)

产品描述
描述
M435-1279 is a UBE2T inhibitor. M435-1279 blocks UBE2T-mediated degradation of RACK1, leading to inhibit the hyperactivation of Wnt/β-catenin signaling pathway.
纯度
97%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:45.0 mg/mL (107.3 mM)
生物活性
In vitro(体外研究)
M435-1279 (0, 2, 4, 8, 16, 31 μM; 48 h) significantly inhibits the growth of AGS, HGC27, and MKN45 cells. M435-1279 (0, 4, 8, 12, 16, 20 μM) inhibits the cell viability with IC50s of 16.8, 11.88, 7.76, 6.93 μM of GES-1, HGC27, AGS MKN45, cells, respectively. M435-1279 (31 nM to 500 μM) binds to UBE2T protein with a KD value of 50.5 μM. M435-1279 (11.88 μM; 48 h) blocks the ubiquitination of RACK1, leading to inhibit the hyperactivation of the Wnt/β-catenin pathway[1].
In vivo(体内研究)
M435-1279 (5 mg/kg/day; intratumor injection; 18 days) slows the tumor growth. M435-1279 induces higher expression of RACK1 proteins, and lower expression of Ki-67 and β-catenin proteins in intratumor tumors[1].