GLUT4-IN-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s 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.

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 .Cell Viability AssayCell Line:CME, K562, KCL-22, MB-231, HS-27 cellsConcentration: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 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 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 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 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.

GLUT4-IN-2 (50 mg/kg; i.p. on day 1–5, 8–12, 15–18) shows antitumor activity in CEM xenograft model.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.

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Others

Other Targets

transporter

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2454113-83-6

385.42

C17H11N3O4S2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (259.46 mM; 超声助溶 (<80°C)

O=C1SC(=CC=2OC=CC2)C(=O)N1CC(=O)NC3=NC=4C=CC=CC4S3

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(-20℃)

With Ice Pack

≥ 2 years