MilliporeSigma™ Calbiochem™ PKM2 Activator III

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.

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