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504537 PKM2 Activator III - CAS 1260074-86-9 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
1260074-86-9C₂₇H₂₆N₄O₄S

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      Description
      OverviewA cell-permeable quinoline-sulfonamide that acts as a potent allosteric PKM2 activator both in cell-free enzymatic assays (AC50 = 17 nM with 40 ng PKM2/200 µL) and in cultures (AC50 = 45 nM in A549 cells) via a high affinity, 2:1 stoichiometric binding, effectively locking PKM2 in an active tetrameric state resistant to known intracellular negative regulators of FBP-activated PKM2 tetramer. PKM2 stimulation by compound treatment is shown to result in decreased serine biosynthesis (by 56%; 500 nM for 24 h) with concomitant increase in serine influx as a compensating mechanism for maintaining cellular serine level necessary for supporting A549 proliferation. Simultaneous PKM2 activation and culture serine withdrawal results in cytostatic A549 growth arrest, but not apoptosis.
      Catalogue Number504537
      Brand Family Calbiochem®
      SynonymsN-(4-(4-(2-Methoxyphenyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide, Pyruvate Kinase M2 Activator III
      References
      ReferencesKung, C., et al. 2012. Chem. Biol. 19, 1187.
      Product Information
      CAS number1260074-86-9
      FormOff-white powder
      Hill FormulaC₂₇H₂₆N₄O₄S
      Chemical formulaC₂₇H₂₆N₄O₄S
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetPKM2
      Purity≥99% 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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      5.04537.0001 04055977244861