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

PKM2 Inhibitor

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 5-(2,5-Dimethyl-1H-pyrrol-1-yl)-2-hydroxybenzoic acid, PKM2 Inhibitor III

Primary Target: pyruvate kinases
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      Overview

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      313701-92-7C₁₃H₁₃NO₃
      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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Catalogue Number GTIN
      533313 0

      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 Protect from light
      +2°C to +8°C
      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.