533313 Pyruvate Kinase Inhibitor III - CAS 313701-92-7 - Calbiochem

533313
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₃H₁₃NO₃ 313701-92-7

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      5.33313.0001
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable pyrrolyl-hydroxybenzoate compound that inhibits fructose-1,6-bisphosphate- (FBP-) dependent activation of pyruvate kinases PKM2 and PKL (IC50 10 to 50 µM), while exhibiting reduced potency against non-FBP-dependent PKM1 activity (81% inhibition of PKM2 vs. 34% inhibition of PKM1 at 30 µM). Lysates from inhibitor-treated (250 µM inhibitor treatment for 6 h) human lung cancer H1299 cells are shown to exhibit significantly reduced PKM2 activity (by 84%) even upon exogenous FBP addition. Inhibitor treatment (Effective conc. 50 to 100 µM) is also demonstrated to enhance cell death of IL-3-dependent murine pro-B lymphocytic FL5.12 and EGFR-signaling-dependent human lung adenocarcinoma HCC827 cultures upon IL-3 withdrawal and EGFR inhibitor treatment, respectively.

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number533313
          Brand Family Calbiochem®
          Synonyms5-(2,5-Dimethyl-1H-pyrrol-1-yl)-2-hydroxybenzoic acid, PKM2 Inhibitor III
          DescriptionPyruvate Kinase Inhibitor III
          References
          ReferencesVander Heiden, M.G., et al. 2010. Biochem. Pharmacol. 79, 1118.
          Product Information
          CAS number313701-92-7
          FormLight brown to brown solid
          Hill FormulaC₁₃H₁₃NO₃
          Chemical formulaC₁₃H₁₃NO₃
          ReversibleY
          Applications
          Biological Information
          Primary Targetpyruvate kinases
          Purity≥95% 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 +2°C to +8°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 2 weeks at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          Pyruvate Kinase Inhibitor III - CAS 313701-92-7 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Vander Heiden, M.G., et al. 2010. Biochem. Pharmacol. 79, 1118.
          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.

          Revision24-June-2016 JSW
          Synonyms5-(2,5-Dimethyl-1H-pyrrol-1-yl)-2-hydroxybenzoic acid, PKM2 Inhibitor III
          DescriptionA cell-permeable pyrrolyl-hydroxybenzoate compound that inhibits fructose-1,6-bisphosphate- (FBP-) dependent activation of pyruvate kinases PKM2 and PKL (IC50 10 to 50 µM), while exhibiting reduced potency against non-FBP-dependent PKM1 activity (81% inhibition of PKM2 vs. 34% inhibition of PKM1 at 30 µM). Lysates from inhibitor-treated (250 µM inhibitor treatment for 6 h) human lung cancer H1299 cells are shown to exhibit significantly reduced PKM2 activity (by 84%) even upon exogenous FBP addition. Inhibitor treatment (Effective conc. 50 to 100 µM) is also demonstrated to enhance cell death of IL-3-dependent murine pro-B lymphocytic FL5.12 and EGFR-signaling-dependent human lung adenocarcinoma HCC827 cultures upon IL-3 withdrawal and EGFR inhibitor treatment, respectively.
          FormLight brown to brown solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number313701-92-7
          Chemical formulaC₁₃H₁₃NO₃
          Purity≥95% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage +2°C to +8°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 2 weeks at -20°C.
          Toxicity Standard Handling
          ReferencesVander Heiden, M.G., et al. 2010. Biochem. Pharmacol. 79, 1118.