85-2076-81　SIRT1/2/3 pan Inhibitor (pan SIRT1/2/3 Inhibitor, 4-(4-(2-Pivalamidoethyl)piperidin-1-yl)thieno[3,2-d]pyrimidine-6-carboxamide) 10mg　217792

特徴

• A thienopyrimidinylcarboxamide that acts as a highly potent, reversible pan sirtuin (SIRT) inhibitor (IC50 = 15, 10, and 33nM 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 > 10uM). Poorly affects hERG and cytochrome P450s (> 50uM). Exhibits desirable stability in microsomal preparations (human CLint = 15.8 uL/min/mg, mouse CLint = 12.7uL/min/mg) and high solubility (297uM), and low LogD (2.73).
• Synonyms:pan SIRT1/2/3 Inhibitor, 4-(4-(2-Pivalamidoethyl)piperidin-1-yl)thieno[3,2-d]pyrimidine-6-carboxamide
• Molecular Formula:C₁₉H₂₇N₅O₂S
• Solubility:DMSO
• Primary Target:SIRT1/2/3
• Purity:≥97% (HPLC)
• Form:Supplied as a pale yellow powder.
• Storage and Stability:Store at 4°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.