Pyruvate Kinase Activator (N-(4-Chloro-3-fluorophenyl)-7-fluoro-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide, PKM2 Activator I)

Blue Ice

372, 8

White powder

A cell-permeable and biologically stable (t1/2 = 277.2 and 117.5 min., respectively, in human and mouse liver microsome preparation) tetrahydroquinoline-sulfonamide that enhances the donor PEP, but not the acceptor ADP, substrate affinity toward pyruvate kinase isoform PKM2 (Km = 0.4 vs. 1.9 mM with or without 10uM activator) and acts as a potent PKM2-selective activator (AC50 = 90nM using rhPKM2; ACmax = 88%), displaying much reduced activity toward PKL (<25% at 57uM) and no effect toward PKM1 or PKR.

Molecular Formula:
C₁₅H₁₁ClF₂N₂O₃S

Molecular Weight:
372.8

Solubility:
DMSO (100mg/ml, clear, colorless solution)

Storage and Stability:
Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.