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Chemical Structure| 724741-75-7 Chemical Structure| 724741-75-7

Structure of STF-31
CAS No.: 724741-75-7

Chemical Structure| 724741-75-7

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STF-31 is a glucose transporter 1 (GLUT1) inhibitor with IC50 of 1 μM.

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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Product Citations

Product Citations

Ding, Wei ; Xie, Lifang ; Wang, Lulu ; Huang, Wenli ; Dong, Yifei ; Fang, Quanlong , et al.

Abstract: Renal ischemia reperfusion injury (IRI) represents a significant factor in perioperative acute kidney injury (AKI), which in turn predisposes to acute renal failure. Dexmedetomidine (Dex) is an anesthetic drug with sedative and analgesic effects, and clinical evidence supports its renoprotective properties. However, the exact molecular mechanism of Dex’s renoprotection remains unclear. Our research specifically focuses on the role of Dex in glycolysis mediated by solute carrier family 2 member 1 (SLC2A1). Here, the renal ischemia/reperfusion (I/R) mouse model and HK-2 oxygen-glucose deprivation/reoxygenation (OGD/R) cell model were established. Pharmacologically, the results showed that Dex ameliorated the injury induced by I/R and OGD/R. Mechanistically, renal IRI elevated SLC2A1 expression, whereas Dex decreased it. STF-31, an inhibitor of SLC2A1, attenuated renal IRI and inhibited glycolysis. Dex inhibited renal IRI in the presence of SLC2A1 but not in the absence. In vitro experiments similarly found this phenomenon. Additionally, Dex promoted SLC2A1 internalization followed by autophagic-lysosomal degradation, as evidenced by immunofluorescence staining and Western blot. In conclusion, Dex has been demonstrated to attenuate renal IRI by inhibiting SLC2A1-mediated glycolysis, which was regulated by SLC2A1 expression, internalization, and lysosomal degradation. The present study presents a novel mechanism by which Dex attenuates renal IRI from a metabolic perspective.

Keywords: Dexmedetomidine ; Renal ischemia/ reperfusion injury ; Glycolysis ; Oxygen glucose deprivation/reoxygenation ; Solute carrier family 2 member 1 ; Renal tubular

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Product Details of STF-31

CAS No. :724741-75-7
Formula : C23H25N3O3S
M.W : 423.53
SMILES Code : O=C(NC1=CC=CN=C1)C2=CC=C(CNS(=O)(C3=CC=C(C(C)(C)C)C=C3)=O)C=C2
English Name :4-((4-(tert-Butyl)phenylsulfonamido)methyl)-N-(pyridin-3-yl)benzamide
MDL No. :MFCD04153828
InChI Key :NGQPRVWTFNBUHA-UHFFFAOYSA-N
Pubchem ID :984333

Safety of STF-31

Isoform Comparison

Biological Activity

Target
  • GLUT1

In Vitro:

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.

In Vivo:

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. Sci Transl Med. 2011 Aug 3;3(94):94ra70.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.81mL

2.36mL

1.18mL

23.61mL

4.72mL

2.36mL

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