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530030 Glutaminase Inhibitor II, BPTES - CAS 314045-39-1 - Calbiochem

A cell-permeable, potent, selective, reversible, and uncompetitive allosteric inhibitor of kidney-type glutaminase (GLS1). Does not affect the activity of liver glutaminase.

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Synonyme: KGA Inhibitor II, N,Nʹ-(5,5ʹ-(2,2ʹ-Thiobis(ethane-2,1-diyl))bis(1,3,4-thiadiazole-5,2-diyl))bis(2-phenylacetamide), Kidney-Type Glutaminase Inhibitor II, GAC Inhibitor II, GLS1 Inhibitor II

Primary Target: kidney-type glutaminase
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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      314045-39-1C₂₄H₂₄N₆O₂S₃
      Description
      OverviewA cell-permeable bis-thiadiazole compound that selectively inhibits GLS1 (IC50 = 60 and 80 nM, respectively, against hKGA and hGAC), but not the liver-type GLS2/LGA (IC50 = 88 µM using hLGA) mitochondrial glutaminase (GA) activity by inducing an inactive GLS1 tetrameric conformation via a 2:1 inhibitor-to-tetramer stoichiometric binding. Shown to induce growth inhibition under aerobic/normoxic (up to 10 µM; 20% O2) and cell death under hypoxic (2 µM; 3% O2) in P493 B-cell lymphoma cultures in vitro and effectively suppress P493 tumor expansion in mice in vivo (12.5 mg/kg or 200 µg/animal via i.p.; q.o.d.).
      Catalogue Number530030
      Brand Family Calbiochem®
      SynonymsKGA Inhibitor II, N,Nʹ-(5,5ʹ-(2,2ʹ-Thiobis(ethane-2,1-diyl))bis(1,3,4-thiadiazole-5,2-diyl))bis(2-phenylacetamide), Kidney-Type Glutaminase Inhibitor II, GAC Inhibitor II, GLS1 Inhibitor II
      References
      ReferencesShukla, K., et al. 2012. J. Med. Chem. 55, 10551.
      Thangavelu, K., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 7705.
      Le, A., et al. 2012. Cell Metab. 15, 110.
      DeLaBarre, B., et al. 2011. Biochemistry 50, 10764.
      Seltzer, M.J., et al. 2010. Cancer Res. 70, 8981.
      Robinson, M.M., et al. 2007. Biochem. J. 406, 407.
      Product Information
      CAS number314045-39-1
      FormYellow powder
      Hill FormulaC₂₄H₂₄N₆O₂S₃
      Chemical formulaC₂₄H₂₄N₆O₂S₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality SegmentMQ100
      Applications
      Biological Information
      Primary Targetkidney-type glutaminase
      Primary Target IC<sub>50</sub>140 and 210 nM in HEK293 cells expressing wt-KGA and F318Y-cKGA, respectively
      Purity≥94% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade ITEM Number
      Bestellnummer GTIN
      530030 0

      Documentation

      Glutaminase Inhibitor II, BPTES - CAS 314045-39-1 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Shukla, K., et al. 2012. J. Med. Chem. 55, 10551.
      Thangavelu, K., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 7705.
      Le, A., et al. 2012. Cell Metab. 15, 110.
      DeLaBarre, B., et al. 2011. Biochemistry 50, 10764.
      Seltzer, M.J., et al. 2010. Cancer Res. 70, 8981.
      Robinson, M.M., et al. 2007. Biochem. J. 406, 407.
      Datenblatt

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision29-April-2014 JSW
      SynonymsKGA Inhibitor II, N,Nʹ-(5,5ʹ-(2,2ʹ-Thiobis(ethane-2,1-diyl))bis(1,3,4-thiadiazole-5,2-diyl))bis(2-phenylacetamide), Kidney-Type Glutaminase Inhibitor II, GAC Inhibitor II, GLS1 Inhibitor II
      DescriptionA cell-permeable bis-thiadiazole compound that selectively inhibits GLS1 (IC50 = 60 and 80 nM, respectively, against hKGA and hGAC), but not the liver-type GLS2/LGA (IC50 = 88 µM using hLGA), mitochondrial glutaminase (GA) activity by inducing an inactive GLS1 tetrameric conformation via a 2:1 inhibitor-to-tetramer stoichiometric binding, non-competitive against glutamine or phosphate binding. B-cell lymphoma line P493 is shown to depend primarily on glutamine metabolism for survival under hypoxic condition and cellular GLS1 inhibtion by BPTES treatment results in cell death (2 µM BPTES & 3% O2 for 4 d), while under aerobic/normoxic condition (20% O2 and up to 10 µM BPTES for 4 d) only growth inhibition is observed. Likewise, intraperitoneal administration (12.5 mg/kg or 200 µg/animal; q.o.d.) is demonstrated to be efficacious in suppressing P493 tumor expansion in mice in vivo.
      FormYellow powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number314045-39-1
      Chemical formulaC₂₄H₂₄N₆O₂S₃
      Structure formulaStructure formula
      Purity≥94% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesShukla, K., et al. 2012. J. Med. Chem. 55, 10551.
      Thangavelu, K., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 7705.
      Le, A., et al. 2012. Cell Metab. 15, 110.
      DeLaBarre, B., et al. 2011. Biochemistry 50, 10764.
      Seltzer, M.J., et al. 2010. Cancer Res. 70, 8981.
      Robinson, M.M., et al. 2007. Biochem. J. 406, 407.