BPTES

• CAT Number: I003115
• CAS Number: 314045-39-1
• Molecular Formula: C24H24N6O2S3
• Molecular Weight: 524.7
• Purity: ≥95%
• Target: Glutaminase
• Solubility: 10 mg/mL in DMSO
• Storage: -20°C
• InChIKey: MDJIPXYRSZHCFS-UHFFFAOYSA-N

BPTES is a potent and selective allosteric inhibitor of kidney-type glutaminase (GLS) that has served as a molecular probe to determine the therapeutic potential of GLS inhibition.IC50: 3.3 uMTarget: Glutaminasein vitro: BPTES is a potent and selective allosteric inhibitor of kidney-type glutaminase (GLS) that has served as a molecular probe to determine the therapeutic potential of GLS inhibition. The truncated derivatives of BPTES inhibits GLS with IC50 of 3.3 uM.in vivo: BPTES exhibits potency and good solubility, attenuates the growth of P493 human lymphoma B cells in a mouse xenograft model.

Reference

1:Combination therapy with BPTES nanoparticles and metformin targets the metabolic heterogeneity of pancreatic cancer. Elgogary A, Xu Q, Poore B, Alt J, Zimmermann SC, Zhao L, Fu J, Chen B, Xia S, Liu Y, Neisser M, Nguyen C, Lee R, Park JK, Reyes J, Hartung T, Rojas C, Rais R, Tsukamoto T, Semenza GL, Hanes J, Slusher BS, Le A.Proc Natl Acad Sci U S A. 2016 Sep 6;113(36):E5328-36. doi: 10.1073/pnas.1611406113. Epub 2016 Aug 24. PMID: 27559084 Free PMC Article2:Glutamine deprivation plus BPTES alters etoposide- and cisplatin-induced apoptosis in triple negative breast cancer cells. Chen L, Cui H, Fang J, Deng H, Kuang P, Guo H, Wang X, Zhao L.Oncotarget. 2016 Aug 23;7(34):54691-54701. doi: 10.18632/oncotarget.10579. PMID: 27419628 Free PMC Article3:Effect of lysine to alanine mutations on the phosphate activation and BPTES inhibition of glutaminase. McDonald CJ, Acheff E, Kennedy R, Taylor L, Curthoys NP.Neurochem Int. 2015 Sep;88:10-4. doi: 10.1016/j.neuint.2014.12.003. Epub 2014 Dec 12. PMID: 25510640 Free PMC Article4:Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors. Shukla K, Ferraris DV, Thomas AG, Stathis M, Duvall B, Delahanty G, Alt J, Rais R, Rojas C, Gao P, Xiang Y, Dang CV, Slusher BS, Tsukamoto T.J Med Chem. 2012 Dec 13;55(23):10551-63. doi: 10.1021/jm301191p. Epub 2012 Nov 30. PMID: 23151085 Free PMC Article5:BPTES inhibition of hGA(124-551), a truncated form of human kidney-type glutaminase. Hartwick EW, Curthoys NP.J Enzyme Inhib Med Chem. 2012 Dec;27(6):861-7. doi: 10.3109/14756366.2011.622272. Epub 2011 Oct 15. PMID: 21999665 6:Novel mechanism of inhibition of rat kidney-type glutaminase by bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide (BPTES). Robinson MM, McBryant SJ, Tsukamoto T, Rojas C, Ferraris DV, Hamilton SK, Hansen JC, Curthoys NP.Biochem J. 2007 Sep 15;406(3):407-14. PMID: 17581113 Free PMC Article