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MilliporeSigma™ Calbiochem™ PKM2 Activator III

Catalog No. 5045370001 Shop All MilliporeSigma Products
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50-453-70001 10 mg
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Catalog No. 50-453-70001 Supplier MilliporeSigma™ Supplier No. 5.04537.0001

Description

A cell-permeable quinoline-sulfonamide that acts as a potent allosteric PKM2 activator both in cell-free enzymatic assays (AC50 = 17nM with 40 ng PKM2/200μL) and in cultures (AC50 = 45nM 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 te

A cell-permeable quinoline-sulfonamide that acts as a potent allosteric PKM2 activator both in cell-free enzymatic assays (AC50 = 17nM with 40 ng PKM2/200μL) and in cultures (AC50 = 45nM 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%; 500nM 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.
TRUSTED_SUSTAINABILITY

Specifications

Color Off-white
Description 99% by HPLC
Target Proteins PKM2
Molecular Formula C27H26N4O4S
Solubility DMSO
Content And Storage Protect from light
Form Powder
Quantity 10 mg
Product Title
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