M435-1279 (C09-1153-017)

M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1In VitroM435-1279 (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 IC 50 s 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 K D 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HGC27, AGS, and MKN45 cells Concentration: 0, 2, 4, 8, 16, 31 μM Incubation Time: 48 h Result: Inhibited the cell growth. Cell Viability AssayCell Line: HGC27, AGS, and MKN45 cells Concentration: 0, 4, 8, 12, 16, 20 μM Incubation Time: Result: Inhibited the cell viability with IC 50 s of 16.8, 11.88, 6.93, 7.76 μM in GES-1, HGC27, MKN45, AGS cells, respectively.In VivoM435-1279 (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/C nude mice CDX model (MKN45 tumor size: 75–100 mm 3 ) Dosage: 5 mg/kg/day Administration: Intratumor injection for 18 days Result: Slowed the tumor growth. Induced higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors.Form:SolidIC50& Target:UBE2T. Specification: 0.98 Molecular Formula: C18H17N3O5S2 Molecular Weight: 419.47