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505487 PKM2 Activator IV, TEPP-46 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
1221186-53-3C₁₇H₁₆N₄O₂S₂

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      Glass bottle 5 mg
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      Description
      OverviewA cell-permeable thienopyrrolopyridazinone that exhibits good aqueous solubility (29.6 µg/mL or 79.5 µM in PBS, pH 7.4) and acts as a potent allosteric PKM2 activator (AC50 = 92 nM; [PKM2] = 0.1 nM) by stabilizing PKM2 tetramer via stoichiometric interaction with FBP-bound PKM2 (2 activator/4 FBP/tetramer) in a similar manner as PKM2 Activator III (Cat. No. 504537). Reprorted to retard human lung carcinoma H1299 proliferation under hypoxia, but not normoxia, condition in cultures (doubling time = 50 and 35 h, respectively, with or without 30 µM TEPP-46; 1% O2) in vitro and impair H1299 tumorigenesis in mice (50 mg/kg/12 h p.o.) in vivo with no apparent toxicity.
      Catalogue Number505487
      Brand Family Calbiochem®
      Synonyms6-((3-Aminophenyl)methyl)-4-methyl-2-methylsulfinylthieno[3,4]pyrrolo[1,3-d]pyridazin-5-one, Pyruvate Kinase M2 Activator IV, ML265, NCGC00186528, TEPP46
      References
      ReferencesAnastasiou, D., et al. 2012. Nat. Chem. Biol. 8, 839.
      Jiang, J.K., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3387.
      Product Information
      CAS number1221186-53-3
      FormWhite solid
      Hill FormulaC₁₇H₁₆N₄O₂S₂
      Chemical formulaC₁₇H₁₆N₄O₂S₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationPKM2 Activator IV, TEPP-46, CAS 1221186-53-3, is a cell-permeable, allosteric PKM2 activator (AC50 = 92 nM) that stabilizes PKM2 tetramer via stoichiometric interaction with FBP-bound PKM2.
      Biological Information
      Primary TargetPKM2
      Purity≥98% 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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      5.05487.0001 04055977243383