GLUT4-IN-2 是一种有效的选择性GLUT4抑制剂，对 GLUT1 和 GLUT4 的IC50s 分别为 11.4 μM 和 6.8 μM。GLUT4-IN-2 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G0/G1 期。GLUT4-IN-2 显示出有效的抗肿瘤活性。
| 生物活性 | GLUT4-IN-2 is a potent and selectiveGLUT4inhibitor withIC50s of 11.4 μM and 6.8 μM forGLUT1andGLUT4, respectively. GLUT4-IN-2 induces cellapoptosisand cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity[1]. |
| IC50& Target[1] | GLUT1 11.4 μM (IC50) | GLUT4 6.8 μM (IC50) |
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体外研究
(In Vitro) | GLUT4-IN-2 (compound F18) induces cell apoptosis and ell cycle arrest at G0/G1phase in CME cells[1].
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[1].
Cell Viability Assay[1] | Cell 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% (CC50) of 1.7, 91.9, 15.3, 45.1, 44.0 μM for CME, K562, KCL-22, MB-231, HS-27 cells, respectively. |
Apoptosis Analysis[1] | Cell 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 Analysis[1] | Cell 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 Analysis[1] | Cell 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 Assay[1] | Cell Line: | CEM cells | | Concentration: | 2.5-100 μM | | Incubation Time: | 48 h | | Result: | Showed cytotoxicity with the IC50s of 1.7, 187.2 μM for CEM, WBCs cells respectively. |
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体内研究
(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[1].
| Animal Model: | 8–10 weeks, SCID mice (CEM xenograft tumor)[1] | | Dosage: | 50 mg/kg | | Administration: | I.p.; administered on day 1-5, 8-12, 15-18 | | Result: | Showed potent antitumor activity in vivo. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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