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Fasentin

CAS No. : 392721-37-8

MCE 站：Fasentin

产品活性：Fasentin 是有效的葡萄糖摄取抑制剂，可抑制 GLUT-1/GLUT-4 转运蛋白。Fasentin 优先抑制 GLUT4 (IC₅₀=68 μM)。Fasentin 是死亡受体刺激 (FAS) 敏化剂，可敏化细胞对 FAS 诱导的细胞死亡。Fasentin 也是诱导肿瘤坏死因子 (TNF) 凋亡配体的敏化剂。Fasentin 阻断癌细胞系中的葡萄糖摄取，并具有抗血管生成活性。

研究领域：Membrane Transporter/Ion Channel

作用靶点：GLUT

In Vitro: Fasentin (0.1-1000 μM; 72?hours) inhibits endothelial, tumour and fibroblast cell growth without inducing cell death.
Fasentin (25-100 μM; 16-24 hours) induces a cell cycle arrest in G0/G1 phase and reduces the cell number in S phase in a dose-dependent manner.
Fasentin (50 μM; 16 hours) alters expression of genes associated with glucose deprivation such as AspSyn and PCK-2.
Fasentin (15, 30, 80 μM; pretreatment 1 hour) induces glucose deprivation, partially blocks glucose uptake in PPC-1, DU145, and U937 cells.
Fasentin (100 μM; 16 hours) does not affect the migratory capability of endothelial cells.
Fasentin (25-100 μM; 16?hours) lowers levels of phospho-ERK in HMECs, indicating a partial inhibition on the ERK signalling pathway, even though the effect is not statistically significant. Fasentin does not inhibit the tyrosine kinase activity of VEGFR2.
Fasentin interacts with a unique site in the intracellular channel of GLUT1.

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