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GLUT4-IN-2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GLUT4-IN-2图片
CAS NO:2454113-83-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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)

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.
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.
分子量

385.42

Formula

C17H11N3O4S2

CAS 号

2454113-83-6

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.