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MilliporeSigma™ Calbiochem™ SIRT1/2/3 pan Inhibitor

Catalog No. 5054790001 Shop All MilliporeSigma Products
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50-547-90001 10 mg
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Catalog No. 50-547-90001 Supplier MilliporeSigma™ Supplier No. 5054790001
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Description

A thienopyrimidinylcarboxamide that acts as a highly potent, reversible pan sirtuin (SIRT) inhibitor (IC50 = 15, 10, and 33nM for SIRT1, 2, and 3, respective

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 > 10μM). Poorly affects hERG and cytochrome P450s (> 50μM). Exhibits desirable stability in microsomal preparations (human CLint = 15.8μL/min/mg, mouse CLint = 12.7μL/min/mg) and high solubility (297μM), and low LogD (2.73).
TRUSTED_SUSTAINABILITY

Specifications

Color Pale Yellow
Description 97% by HPLC
Target Proteins SIRT1/2/3
Molecular Formula C19H27N5O2S
Solubility DMSO
Content And Storage Protect from light
Form Powder
Quantity 10 mg
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