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Description

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).