GLUT4-IN-2

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 activity In Vitro GLUT4-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 Vivo GLUT4-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:Solid IC50& Target:GLUT1 11.4 μM (IC 50 ) GLUT4 6.8 μM (IC 50 )

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet