Fasentin is an effective inhibitor of glucose uptake, targeting GLUT-1/GLUT-4 transport proteins. It preferentially inhibits GLUT4 over GLUT1, with an IC50 value of 68 μM. Fasentin acts as a sensitizer to FAS, making cells more susceptible to FAS-induced cell death. It also serves as a sensitizer for the TNF apoptosis-inducing ligand. Fasentin can block glucose uptake in cancer cell lines and exhibits anti-angiogenic activity[1][2][3]. When cells are treated with Fasentin at concentrations ranging from 25-100 μM for 16-24 hours, it induces a cell cycle arrest at the G0/G1 phase and reduces the number of cells in the S phase in a dose-dependent manner[1]. At a concentration of 50 μM, a 16-hour treatment with Fasentin alters the expression of genes associated with glucose deprivation, such as AspSyn and PCK-2. Furthermore, pre-treating cells for 1 hour at concentrations of 15, 30, and 80 μM, Fasentin can induce glucose deprivation and partially block glucose uptake in PPC-1, DU145, and U937 cells[2].
Fasentin 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Peripheral blood mononuclear cells (PBMCs)
25 μM
6 hours
Inhibition of GLUT-1-mediated glucose internalization, reduction of PKM2 nuclear translocation, and down-regulation of pro-inflammatory cytokine expression
Cardiovasc Res. 2023 Dec 19;119(16):2653-2662
A549 cells
10 μM
24 hours
To investigate the effect of Fasentin on Nrf2 protein expression, results showed that Fasentin significantly increased the expression level of Nrf2 protein.
Int J Mol Sci. 2021 Jun 19;22(12):6582
A549 cells
10 μM
6 hours
To investigate the effect of Fasentin on the expression of glucose transporters and metabolic enzymes, results showed that Fasentin increased the expression levels of these proteins.
Int J Mol Sci. 2021 Jun 19;22(12):6582
GSC28 cells
50 µM
24 hours
Inhibits GLUT1 expression but does not alter TUBB4 expression
Cancers (Basel). 2019 Sep 5;11(9):1308
GSC33 cells
50 µM
24 hours
Inhibits GLUT1 expression but does not alter TUBB4 expression
Cancers (Basel). 2019 Sep 5;11(9):1308
GLC-36
50.0 and 100.0 µM
4 days
analyze cell proliferation and survival, significant negative impact on cell numbers at high concentrations
Cancers (Basel). 2023 Feb 23;15(5):1415
GLC-2
50.0 and 100.0 µM
4 days
analyze cell proliferation and survival, significant negative impact on cell numbers at high concentrations
Cancers (Basel). 2023 Feb 23;15(5):1415
QPG-1
50.0 and 100.0 µM
4 days
analyze cell proliferation and survival, significant negative impact on cell numbers at high concentrations
Cancers (Basel). 2023 Feb 23;15(5):1415
BON-1
50.0 and 100.0 µM
4 days
analyze cell proliferation and survival, significant negative impact on cell numbers at high concentrations
Cancers (Basel). 2023 Feb 23;15(5):1415
human gingival fibroblasts (HGF)
25, 50, 100 µM
72 hours
To evaluate the effect of Fasentin on cell proliferation, results showed that Fasentin inhibited HGF proliferation with an IC50 of 111.2 ± 27.0 µM.
Sci Rep. 2020 Apr 9;10(1):6132
human cervix adenocarcinoma cells (HeLa)
25, 50, 100 µM
72 hours
To evaluate the effect of Fasentin on cell proliferation, results showed that Fasentin inhibited HeLa proliferation with an IC50 of 31.9 ± 1.4 µM.
Sci Rep. 2020 Apr 9;10(1):6132
human breast carcinoma cells (MCF7)
25, 50, 100 µM
72 hours
To evaluate the effect of Fasentin on cell proliferation, results showed that Fasentin inhibited MCF7 proliferation with an IC50 of 34.7 ± 4.0 µM.
Sci Rep. 2020 Apr 9;10(1):6132
human breast carcinoma cells (MDA-MB-231)
25, 50, 100 µM
72 hours
To evaluate the effect of Fasentin on cell proliferation, results showed that Fasentin inhibited MDA-MB-231 proliferation with an IC50 of 26.3 ± 4.8 µM.
Sci Rep. 2020 Apr 9;10(1):6132
bovine aortic endothelial cells (BAEC)
25, 50, 100 µM
72 hours
To evaluate the effect of Fasentin on cell proliferation, results showed that Fasentin inhibited BAEC proliferation with an IC50 of 42.7 ± 9.5 µM.
Sci Rep. 2020 Apr 9;10(1):6132
human umbilical vein endothelial cells (HUVEC)
25, 50, 100 µM
72 hours
To evaluate the effect of Fasentin on cell proliferation, results showed that Fasentin inhibited HUVEC proliferation with an IC50 of 27.6 ± 3.7 µM.
Sci Rep. 2020 Apr 9;10(1):6132
human microvascular endothelial cells (HMEC)
25, 50, 100 µM
72 hours
To evaluate the effect of Fasentin on cell proliferation, results showed that Fasentin inhibited HMEC proliferation with an IC50 of 27.9 ± 14.5 µM.
Sci Rep. 2020 Apr 9;10(1):6132
AtT-20/D16:16 cells
1 μM and 40 μM
3 hours
Fasentin inhibited baseline and CRH-mediated glucose uptake
Mol Cell Endocrinol. 2018 Jul 15;470:105-114
human cardiac progenitor cells (hCPCs)
1 μM
72 hours
Fasentin restored hCPC viability and tube-forming ability by specifically inhibiting GLUT1 and reduced the expression of mitochondrial fission-related proteins Fis1 and Drp1.
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