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Pyruvate Kinase Activator
N-(4-Chloro-3-fluorophenyl)-7-fluoro-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide, PKM2 Activator I
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 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.
产品信息
Form White powder
Molar mass 372.8
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥98% by HPLC
Solubility DMSO
Chemical formula C15H11ClF2N2O3S
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |