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

504537
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Overview

Key Spec Table

CAS #Empirical Formula
1260074-86-9C₂₇H₂₆N₄O₄S

Products

Catalogue NumberPackaging Qty/Pack
5045370001 Glass bottle 10 mg
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
5045370001 04055977244861