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

530030
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₄H₂₄N₆O₂S₃ 314045-39-1

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      5.30030.0001
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          Glass bottle 10 mg
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          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®
          SynonymsN,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, KGA 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
          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

          Documentation

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

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          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.
          Data Sheet

          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
          SynonymsN,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, KGA 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 -20°C
          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.
          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.