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505479 SIRT1/2/3 pan Inhibitor - CAS 1431411-60-7 - Calbiochem

505479
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Overview

Key Spec Table

CAS #Empirical Formula
1431411-60-7C₁₉H₂₇N₅O₂S

Products

Catalogue NumberPackaging Qty/Pack
5.05479.0001 Glass bottle 10 mg
Description
OverviewA 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 µM). Poorly affects hERG and cytochrome P450s (> 50 µM). Exhibits desirable stability in microsomal preparations (human CLint = 15.8 µL/min/mg, mouse CLint = 12.7 µL/min/mg) and high solubility (297 µM), and low LogD (2.73).
Catalogue Number505479
Brand Family Calbiochem®
Synonymspan SIRT1/2/3 Inhibitor, 4-(4-(2-Pivalamidoethyl)piperidin-1-yl)thieno[3,2-d]pyrimidine-6-carboxamide
References
ReferencesDisch, J.S., et al. 2013. J. Med. Chem. 57, 1275.
Product Information
CAS number1431411-60-7
FormPale yellow powder
Hill FormulaC₁₉H₂₇N₅O₂S
Chemical formulaC₁₉H₂₇N₅O₂S
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Biological Information
Primary TargetSIRT1/2/3
Purity≥97% by HPLC
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
5.05479.0001 04055977243871