Pyruvate Kinase Activator - Calbiochem

General Description

A cell-permeable (P_app x 10⁶ = 9.38 and 7.91 cm/s, respectively, for "A-B" and "B-A" in Caco-2 permeability assay) and biologically stable (t_1/2 = 277.2 and 117.5 min., respectively, using human and mouse liver microsome preparation) tetrahydroquinoline-sulfonamide that enhances the donor PEP (phosphoenolpyruvate), but not the acceptor ADP, substrate affinity toward PK (pyruvate kinase) isoform PKM2 (K_m = 0.4 vs. 1.9 mM with or without 10 μM activator) and acts as a potent PKM2-selective activator (AC₅₀ = 90 nM using rhPKM2; AC_max = 88%), displaying much reduced activity toward PKL (≤25% at 57 μM) and no effect toward PKM1 or PKR.