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

533313
  
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      Overview

      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
      Biological Information
      Primary Targetpyruvate kinases
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Catalogue Number GTIN
      533313 0