Key Documents

COA/COQ

5.05479

SIRT1/2/3 pan Inhibitor

Name: SIRT1/2/3 pan Inhibitor
Brand: MM

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

Sign Into View Organizational & Contract Pricing

Select a Size

All Photos(1)

About This Item

Empirical Formula (Hill Notation):

C₁₉H₂₇N₅O₂S

CAS Number:

1431411-60-7

Molecular Weight:

389.51

MDL number:

MFCD00149973

UNSPSC Code:

12352200

NACRES:

NA.77

Assay

≥97% (HPLC)

Quality Level

100

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 CL_int = 15.8 µL/min/mg, mouse CL_int = 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 Code

11 - Combustible Solids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Global Trade Item Number

SKU	GTIN
5.05479.0001	04055977243871

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service