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 (AC 50 = 17nM with 40 ng PKM2/200μL) and in cultures (AC 50 = 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.