STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM. STF-31completely suppressed the glucose uptake activity and induced apoptosis in GLUT1 expressing myeloma cells. Moreover, STF-31 synergistically enhanced the cell death induced by melphalan, doxorubicin, and bortezomib[3]. STF-31 (0.01-10 μM; 10 days) is specifically toxic to RCC4 cells, whereas RCC4/VHL cells are relatively unaffected. RCC4/VHL cells treated with STF-31 (5 μM; 10 days) largely recovery, whereas RCC4 cells under the same conditions does not. STF-31 (1.25-5 μM; 3 days) does not induce autophagy, apoptosis, or DNA damage. STF-31 causes a necrotic cell death. Soluble analog of STF-31 (11.6 mg/kg; i.p.) treatment delays tumor growth in mice with VHL-deficient RCC tumor xenografts[4]. STF-31 (10 mg/kg; i.p.; twice daily for 2 days, followed by once daily for another 3 days) does not affect normal mice body weight, behavior, and ERG responses. STF-31 reduces light-induced CX3CR1gfp/+ mice microglial activation and retinal degeneration[5].
STF-31 细胞实验
Cell Line
Concentration
Treated Time
Description
References
ACHN cells (VHL shRNA)
5 µM
10 days
Evaluate the toxicity of STF-31 to VHL shRNA cells, results showed STF-31 significantly reduced the viability of ACHN cells.
Sci Transl Med. 2011 Aug 3;3(94):94ra70.
RCC4/VHL cells (VHL wild-type)
5 µM
10 days
Evaluate the toxicity of STF-31 to VHL wild-type cells, results showed STF-31 had minimal effect on the viability of RCC4/VHL cells.
Sci Transl Med. 2011 Aug 3;3(94):94ra70.
Human microvascular endothelial cells (HMEC)
100 µM
16 hours
To test the effect of STF-31 on tube formation in HMECs, results showed that STF-31 failed to inhibit tube formation.
Sci Rep. 2020 Apr 9;10(1):6132.
Human embryonic stem cells (hESCs)
2.5 µM
24-72 hours
Evaluate the toxic effects of STF-31 on hESCs, results showed STF-31 significantly reduced cell viability within 72 hours
Stem Cells Transl Med. 2015 May;4(5):483-93.
Human induced pluripotent stem cells (hiPSCs)
2.5 µM
24-72 hours
Evaluate the toxic effects of STF-31 on hiPSCs, results showed STF-31 significantly reduced cell viability to 10% within 72 hours
Stem Cells Transl Med. 2015 May;4(5):483-93.
RCC4 cells (VHL-deficient)
5 µM
4 days
Evaluate the toxicity of STF-31 to VHL-deficient cells, results showed STF-31 significantly reduced the viability of RCC4 cells.
Sci Transl Med. 2011 Aug 3;3(94):94ra70.
GLC-36
0.1, 1.0, 5.0, 10.0, 50.0, 100.0 µM
4 days
GLC-36 cells showed partial resistance to STF-31 at intermediate concentrations but were still affected at high concentrations.
Cancers (Basel). 2023 Feb 23;15(5):1415.
GLC-2
0.1, 1.0, 5.0, 10.0, 50.0, 100.0 µM
4 days
STF-31 treatment significantly reduced cell numbers in GLC-2 cells, even at low concentrations of 0.1 µM.
Cancers (Basel). 2023 Feb 23;15(5):1415.
QPG-1
0.1, 1.0, 5.0, 10.0, 50.0, 100.0 µM
4 days
STF-31 treatment significantly reduced cell numbers in QPG-1 cells, even at low concentrations of 0.1 µM.
Cancers (Basel). 2023 Feb 23;15(5):1415.
BON-1
0.1, 1.0, 5.0, 10.0, 50.0, 100.0 µM
4 days
STF-31 treatment significantly reduced cell numbers in GLC-2 and QPG-1 cells, even at low concentrations of 0.1 µM. GLC-36 cells showed partial resistance at intermediate concentrations, while Bon-1 cells exhibited high resistance.
Cancers (Basel). 2023 Feb 23;15(5):1415.
N27 cells
0.5 µM
48 hours
Inhibition of GLUT-like glucose transport significantly reduced PQ-induced cell death
Mol Neurobiol. 2017 Jul;54(5):3825-3842.
Human induced pluripotent stem cells (hiPSCs)
2.5 µM
48-72 hours
Evaluate the toxic effect of STF-31 on hiPSCs, showing 80% cell death within 48 hours and almost complete death within 72 hours
Stem Cell Reports. 2014 Jun 6;3(1):185-203.
Human embryonic stem cells (hESCs)
2.5 µM
48-72 hours
Evaluate the toxic effect of STF-31 on hESCs, showing 80% cell death within 48 hours and almost complete death within 72 hours
Stem Cell Reports. 2014 Jun 6;3(1):185-203.
HCT116 cells
200 nM
72 hours
To evaluate the growth inhibitory effect of STF-31 analogue compound 146 on HCT116 cells, results showed that compound 146 effectively inhibited cell growth.
ACS Chem Biol. 2014 Oct 17;9(10):2247-54.
HESC-derived cardiomyocytes (hESC-CMs)
2.5 µM
72 hours
Evaluate the effect of STF-31 on hESC-CMs, showing no adverse effects
Stem Cell Reports. 2014 Jun 6;3(1):185-203.
Human fibroblasts (hFibs)
2.5 µM
72 hours
Evaluate the effect of STF-31 on hFibs, showing no adverse effects
Stem Cell Reports. 2014 Jun 6;3(1):185-203.
Human mesenchymal stem cells (hMSCs)
2.5 µM
72 hours
Evaluate the effect of STF-31 on hMSCs, showing no adverse effects
Stem Cell Reports. 2014 Jun 6;3(1):185-203.
STF-31 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
786-O and ACHN xenograft models
Intraperitoneal injection
11.6 mg/kg (first 3 days), followed by 7.8 mg/kg (7-9 days)
Once or twice daily for 10-14 days
Evaluate the antitumor effect of STF-31 analog in vivo, results showed STF-31 significantly delayed tumor growth without toxicity to normal tissues.
搜索
