SIRT1/2/3 pan Inhibitor – Calbiochem

Descrição detalhada : A thienopyrimidinylcarboxamide that acts as a highly potent, reversible pan sirtuin (SIRT) inhibitor (IC50 = 15, 10, and 33 nM for SIRT1, 2, and 3, respectively). Shown to bind to the SIRT catalytic site and occupy both the nicotinamide C-pocket and acetyl lysine substrate channel. Exhibits high selectivity over a panel of protein kinases, nuclelar receptors, GPCRs, and ion-channels (IC50 >10 microM). Poorly affects hERG and cytochrome P450s (>50 microM). Exhibits desirable stability in microsomal preparations (human CLint = 15.8 microL/min/mg, mouse CLint = 12.7 microL/min/mg) and high solubility (297 microM), and low LogD (2.73).
Sinónimos : SIRT1/2/3 pan Inhibitor - Calbiochem; 4-(4-(2-Pivalamidoethyl)piperidin-1-yl)thieno[3,2-d]pyrimidine-6-carboxamide, pan SIRT1/2/3 Inhibitor; pan SIRT1/2/3 Inhibitor, 4-(4-(2-Pivalamidoethyl)piperidin-1-yl)thieno[3,2-d]pyrimidine-6-carboxamide
Fórmula molecula r: C19H27N5O2S
Armazenamento : 2-8C; 2-8C
Embalagem : 1X1EA