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Merck

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:
1431411-60-7
Molecular Weight:
389.51
MDL number:
MFCD00149973
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥97% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze, protect from light

Key Documents

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assay

≥97% (HPLC)

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

Quality Level

100

Related Categories

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
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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Global Trade Item Number

SKUGTIN
5.05479.000104055977243871

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