GLUT4-IN-2 (C09-1135-180)

GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC 50 s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4 , respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activityIn VitroGLUT4-IN-2 (compound F18) induces cell apoptosis and ell cycle arrest at G0/G1phase in CME cells. GLUT4-IN-2 (10 µM; 6 h) decreases the expression of mTOR and CDK2, but increases the expression of GRP78, and cleaved caspase 3 proteins. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: CME, K562, KCL-22, MB-231, HS-27 cells Concentration: 1-100 µM Incubation Time: 48 h Result: Showed potent cytotoxicity with cytotoxic concentration 50% (CC 50 ) of 1.7, 91.9, 15.3, 45.1, 44.0 µM for CME, K562, KCL-22, MB-231, HS-27 cells, respectively. Apoptosis AnalysisCell Line: CEM cells Concentration: 1.7 µM Incubation Time: 24 h Result: Induced cell apoptosis with the percentage of apoptotic cells in the late and early apoptosis region was 55.87% and 1.38%, respectively. Cell Cycle AnalysisCell Line: CEM cells Concentration: 10, 25, 50 µM Incubation Time: 72 h Result: Induced cell cycle arrest at G0/G1phase in a dose-dependent manner. Western Blot AnalysisCell Line: CEM cells Concentration: 10 µM Incubation Time: 6 h Result: Decreased the phosphorylation of mTOR and CDK2 proteins and increased the expression of GRP78, and cleaved caspase 3. Cell Cytotoxicity AssayCell Line: CEM cells Concentration: 2.5-100 µM Incubation Time: 48 h Result: Showed cytotoxicity with the IC 50 s of 1.7, 187.2 µM for CEM, WBCs cells respectively.In VivoGLUT4-IN-2 (50 mg/kg; i.p. on day 1–5, 8–12, 15–18) shows antitumor activity in CEM xenograft model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 8–10 weeks, SCID mice (CEM xenograft tumor) Dosage: 50 mg/kg Administration: I.p.; administered on day 1-5, 8-12, 15-18 Result: Showed potent antitumor activity in vivo.Form:SolidIC50& Target:GLUT1 11.4 μM (IC 50 ) GLUT4 6.8 μM (IC 50 ). Molecular Formula: C17H11N3O4S2 Molecular Weight: 385.42