Pyruvate Kinase Activator - Calbiochem C화학적 특성, 용도, 생산
일반 설명
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 μM activator) and acts as a potent PKM2-selective activator (AC50 = 90 nM using rhPKM2; ACmax = 88%), displaying much reduced activity toward PKL (≤25% at 57 μM) and no effect toward PKM1 or PKR.
Pyruvate Kinase Activator - Calbiochem 준비 용품 및 원자재