5.05479
SIRT1/2/3 pan Inhibitor
Synonym(s):
SIRT1/2/3 pan Inhibitor, 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
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About This Item
Empirical Formula (Hill Notation):
C19H27N5O2S
CAS Number:
Molecular Weight:
389.51
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥97% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
assay
≥97% (HPLC)
Quality Segment
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow
solubility
DMSO: 10 mg/mL
storage temp.
2-8°C
General 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 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).
Biochem/physiol Actions
Primary Target
SIRT1/2/3
SIRT1/2/3
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Disch, J.S., et al. 2013. J. Med. Chem.57, 1275.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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