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Beschreibung

A cell-permeable (Papp x 106 = 9.38 and 7.91 cm/s, respectively, for ",A-B", and ",B-A", in Caco-2 permeability assay) and biologically stable (t1/2 = 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 (Km = 0.4 vs. 1.9 mM with or without 10 microM activator) and acts as a potent PKM2-selective activator (AC50 = 90 nM using rhPKM2, ACmax = 88%), displaying much reduced activity toward PKL (&le,25% at 57 microM) and no effect toward PKM1 or PKR., 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 10 microM activator) and acts as a potent PKM2-selective activator (AC50 = 90 nM using rhPKM2, ACmax = 88%), displaying much reduced activity toward PKL (&le,25% at 57 microM) and no effect toward PKM1 or PKR.