GSK264220A，25MG，SML2931-25MG，Sigma

Biochem/physiol Actions

GSK264220A is a potent, active site-targeting, covalent inhibitor against endothelial lipase (EL or LIPG; IC₅₀ = 130 nM) and lipoprotein lipase (LPL or LIPD; IC₅₀ = 100 nM). GSK264220A reduces NeuT expression - or CoCl₂ treatment-induced intracellular triacylglycerol & lipid droplets (TAG & LD) increase in MCF-7 (16 & 32 nM) and suppresses LPL-depenent melanoma survival (by ~50% at 18.75 μM; WM852, WM1361). When applied in mice in vivo (30 mg/kg ip.), GSK264220A21 enhances lipid nanoparticles-mediated siRNAs delivery & gene-silencing efficacy.
Potent, active site-targeting, covalent inhibitor against endothelial lipase (EL, LIPG) and lipoprotein lipase (LPL, LIPD) in vitro and in vivo.