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5MPN

CAS No. : 47208-82-2

MCE 站：5MPN

产品活性：5MPN 是一种一流、有效、具有口服活性和选择性的 6-磷酸果糖-2激酶/果糖-2,6-二磷酸酶4 (PFKFB4)抑制剂。5MPN 是 F6P 结合位点的竞争性抑制剂 (K_i=8.6 μM)。5MPN 不抑制 PFK-1 或 PFKFB3。5MPN 抑制糖代谢可能对晚期实体癌产生有利的治疗指标。

研究领域：Others

作用靶点：Others

In Vitro: 5MPN (0~30 μM; 24 hours; H460 cells) inhibits the expression of PFKFB4.
5MPN (0~50 μM; 0~72 hours; H460 NSCLC cells) first reduces the intracellular concentration of F2,6BP, glycolysis ａnd ATP, which in turn results in a reduction in cell proliferation.
5MPN (0 ａnd 10 μM; 6, 12 ａnd 24 hours; H460 cells) induces cells apoptosis.
5MPN (0 ａnd 10 μM; 6, 12 ａnd 24 hours; H460 cells) arrests cell cycle progression.
5MPN (0.1, 1 or 10 µM) significantly inhibits PFKFB4 activity. 5MPN (H460 cells) leads to a dose-dependent decrease in the intracellular F2,6BP concentration. 5MPN (0~30 μM; over 48 hours; H460, H1299, H441, H522 ａnd A549 cells) makes a dose-dependent reduction in cells growth. 5MPN (0~30 μM; 24 hours; H460 cells) inhibits PFKFB4 expression causing the observed reduction in H460 cell proliferation. 5MPN causes a G1 arrest in LLC cells in vitro similar to H460 cells.

In Vivo: 5MPN (120 mg/kg; p.o.) suppresses the growth of Lewis lung carcinomas (LLC) grown in syngeneic mice ａnd H460 human lung adenocarcinoma xenografts grown in athymic mice without affecting body weight.
5MPN causes a reduction in Ki67-positive cells in the LLC xenografts suggesting that 5MPN may be reducing cell cycle progression in vivo.

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