GLUT4-IN-2

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^[1].

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].
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].

References:
[1]. Tilekar K,et al. Structure guided design and synthesis of furyl thiazolidinedione derivatives as inhibitors of GLUT 1 and GLUT 4, and evaluation of their anti-leukemic potential. Eur J Med Chem. 2020 Sep 15;202:112603.

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。