WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H407169
CAS#: 724741-75-7
Description: STF31 is a potent glucose transporter 1 (GLUT1). STF31 selectively kills RCCs by specifically targeting glucose uptake through GLUT1 and exploiting the unique dependence of these cells on GLUT1 for survival. Treatment with STF31 inhibits the growth of RCCs by binding GLUT1 directly and impeding glucose uptake in vivo without toxicity to normal tissue. STF-31 is toxic to hPSCs and efficient for selective elimination of hPSCs from mixed cultures.
Hodoodo Cat#: H407169
Name: STF31
CAS#: 724741-75-7
Chemical Formula: C23H25N3O3S
Exact Mass: 423.16
Molecular Weight: 423.530
Elemental Analysis: C, 65.23; H, 5.95; N, 9.92; O, 11.33; S, 7.57
Synonym: STF31; STF-31; STF 31.
IUPAC/Chemical Name: 4-(((4-(tert-butyl)phenyl)sulfonamido)methyl)-N-(pyridin-3-yl)benzamide
InChi Key: NGQPRVWTFNBUHA-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H25N3O3S/c1-23(2,3)19-10-12-21(13-11-19)30(28,29)25-15-17-6-8-18(9-7-17)22(27)26-20-5-4-14-24-16-20/h4-14,16,25H,15H2,1-3H3,(H,26,27)
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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM. |
| In vitro activity: | Data indicate that STF-31 targets NAMPT, the enzyme that catalyzes the rate-limiting step in the conversion of nicotinamide to NAD+ in one of the NAD+ salvage pathways. Further support of this mechanism is found in two separate studies that were published while our manuscript was under review. Altogether, these data provide evidence that STF-31-mediated toxicity is due to the inhibition of the NAMPT-mediated NAD+ salvage pathway. Additionally, this study provides evidence that the toxic effects mediated by STF-31 in hPSCs can be attributed to depletion of NAD+, not inhibition of glucose transport. Reference: Stem Cells Transl Med. 2015 May; 4(5): 483–493. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4414215/ |
| In vivo activity: | Intraperitoneal injection of STF31 (10 mg/kg, for 5 days) in normal mice did not affect their body weight, behavior, and ERG responses (Additional file 1: Figure S3A, B). The treatment did not induce any retinal cell death (Additional file 1: Figure S3C). Massive photoreceptor loss (Fig. 9a-b, e) and microglial activation (Fig. 9f-g, j) were observed 4 days after light exposure. STF31 treatment improved photoreceptor survival and reduced microglial activation (Fig. 9). The treatment with vehicle (DMSO) did not show any protective effect (Fig. 9). SD-OCT examination showed improvement in both retinal structure and thickness, particularly the outer retinal layers (from ONL to IS/OS, Additional file 1: Figure S4E, G) following STF31 treatment (Additional file 1: Figure S4).The treatment did not significantly improve the thickness of the inner retina (from NFL/GL to OPL, Additional file 1: Figure S4E, F). Reference: Mol Neurodegener. 2019; 14: 2. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6329071/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.1 | 75.84 |
The following data is based on the product molecular weight 423.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Kropp EM, Oleson BJ, Broniowska KA, Bhattacharya S, Chadwick AC, Diers AR, Hu Q, Sahoo D, Hogg N, Boheler KR, Corbett JA, Gundry RL. Inhibition of an NAD⁺ salvage pathway provides efficient and selective toxicity to human pluripotent stem cells. Stem Cells Transl Med. 2015 May;4(5):483-93. doi: 10.5966/sctm.2014-0163. Epub 2015 Apr 1. PMID: 25834119; PMCID: PMC4414215. 2. Adams DJ, Ito D, Rees MG, Seashore-Ludlow B, Puyang X, Ramos AH, Cheah JH, Clemons PA, Warmuth M, Zhu P, Shamji AF, Schreiber SL. NAMPT is the cellular target of STF-31-like small-molecule probes. ACS Chem Biol. 2014 Oct 17;9(10):2247-54. doi: 10.1021/cb500347p. Epub 2014 Aug 7. PMID: 25058389; PMCID: PMC4201331. 3. Wang L, Pavlou S, Du X, Bhuckory M, Xu H, Chen M. Glucose transporter 1 critically controls microglial activation through facilitating glycolysis. Mol Neurodegener. 2019 Jan 11;14(1):2. doi: 10.1186/s13024-019-0305-9. PMID: 30634998; PMCID: PMC6329071. 4. Pingitore A, Ruz-Maldonado I, Liu B, Huang GC, Choudhary P, Persaud SJ. Dynamic Profiling of Insulin Secretion and ATP Generation in Isolated Human and Mouse Islets Reveals Differential Glucose Sensitivity. Cell Physiol Biochem. 2017;44(4):1352-1359. doi: 10.1159/000485532. Epub 2017 Nov 30. PMID: 29186709. |
| In vitro protocol: | 1. Kropp EM, Oleson BJ, Broniowska KA, Bhattacharya S, Chadwick AC, Diers AR, Hu Q, Sahoo D, Hogg N, Boheler KR, Corbett JA, Gundry RL. Inhibition of an NAD⁺ salvage pathway provides efficient and selective toxicity to human pluripotent stem cells. Stem Cells Transl Med. 2015 May;4(5):483-93. doi: 10.5966/sctm.2014-0163. Epub 2015 Apr 1. PMID: 25834119; PMCID: PMC4414215. 2. Adams DJ, Ito D, Rees MG, Seashore-Ludlow B, Puyang X, Ramos AH, Cheah JH, Clemons PA, Warmuth M, Zhu P, Shamji AF, Schreiber SL. NAMPT is the cellular target of STF-31-like small-molecule probes. ACS Chem Biol. 2014 Oct 17;9(10):2247-54. doi: 10.1021/cb500347p. Epub 2014 Aug 7. PMID: 25058389; PMCID: PMC4201331. |
| In vivo protocol: | 1. Wang L, Pavlou S, Du X, Bhuckory M, Xu H, Chen M. Glucose transporter 1 critically controls microglial activation through facilitating glycolysis. Mol Neurodegener. 2019 Jan 11;14(1):2. doi: 10.1186/s13024-019-0305-9. PMID: 30634998; PMCID: PMC6329071. 2. Pingitore A, Ruz-Maldonado I, Liu B, Huang GC, Choudhary P, Persaud SJ. Dynamic Profiling of Insulin Secretion and ATP Generation in Isolated Human and Mouse Islets Reveals Differential Glucose Sensitivity. Cell Physiol Biochem. 2017;44(4):1352-1359. doi: 10.1159/000485532. Epub 2017 Nov 30. PMID: 29186709. |
1: Kropp EM, Oleson BJ, Broniowska KA, Bhattacharya S, Chadwick AC, Diers AR, Hu
Q, Sahoo D, Hogg N, Boheler KR, Corbett JA, Gundry RL. Inhibition of an NAD⁺
salvage pathway provides efficient and selective toxicity to human pluripotent
stem cells. Stem Cells Transl Med. 2015 May;4(5):483-93. doi:
10.5966/sctm.2014-0163. Epub 2015 Apr 1. PubMed PMID: 25834119; PubMed Central
PMCID: PMC4414215.
2: Boheler KR, Bhattacharya S, Kropp EM, Chuppa S, Riordon DR, Bausch-Fluck D,
Burridge PW, Wu JC, Wersto RP, Chan GC, Rao S, Wollscheid B, Gundry RL. A human
pluripotent stem cell surface N-glycoproteome resource reveals markers,
extracellular epitopes, and drug targets. Stem Cell Reports. 2014 Jun
6;3(1):185-203. doi: 10.1016/j.stemcr.2014.05.002. eCollection 2014 Jul 8. PubMed
PMID: 25068131; PubMed Central PMCID: PMC4110789.
3: Adams DJ, Ito D, Rees MG, Seashore-Ludlow B, Puyang X, Ramos AH, Cheah JH,
Clemons PA, Warmuth M, Zhu P, Shamji AF, Schreiber SL. NAMPT is the cellular
target of STF-31-like small-molecule probes. ACS Chem Biol. 2014 Oct
17;9(10):2247-54. doi: 10.1021/cb500347p. Epub 2014 Aug 7. PubMed PMID: 25058389;
PubMed Central PMCID: PMC4201331.
4: Chan DA, Sutphin PD, Nguyen P, Turcotte S, Lai EW, Banh A, Reynolds GE, Chi
JT, Wu J, Solow-Cordero DE, Bonnet M, Flanagan JU, Bouley DM, Graves EE, Denny
WA, Hay MP, Giaccia AJ. Targeting GLUT1 and the Warburg effect in renal cell
carcinoma by chemical synthetic lethality. Sci Transl Med. 2011 Aug
3;3(94):94ra70. doi: 10.1126/scitranslmed.3002394. PubMed PMID: 21813754; PubMed
Central PMCID: PMC3683134.
