The SIRT1/2 Inhibitor IV, Cambinol, also referenced under CAS 14513-15-6, controls the biological activity of SIRT1/2. This small molecule/inhibitor is primarily used for Cell Structure applications.
Synonym(s):
SIRT1/2 Inhibitor IV, Cambinol, 5-(2-Hydroxy-naphthalen-1-ylmethyl)-6-phenyl-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one, NSC-112546, SIRT1 Inhibitor II, SIRT2 Inhibitor VI
A cell-permeable β-naphthol compound that inhibits the NAD-dependent deacetylase activity of hSIRT1 and hSIRT2 (IC50 = 56 µM and 59 µM, respectively) in a substrate-, but not NAD-, competitive manner. It inhibits SIRT5 deacetylase activity only at much higher concentrations (IC50 >300 µM) and exhibits no inhibition against class I and II HDACs. Cambinol-induced apoptosis in BCL6-expressing Burkitt lymphoma cell lines has been attributed to the hyperacetylation of BCL6 and p53. Shown to effectively inhibit xenografted Daudi Burkitt lymphoma growth in mice in vivo.
Biochem/physiol Actions
Cell permeable: yes
Primary Target hSIRT1 and hSIRT2
Product does not compete with ATP.
Reversible: no
Target IC50: 56 µM and 59 µM against the NAD-dependent deacetylase activity of hSIRT1 and hSIRT2, respectively
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Other Notes
Heltweg, B., et al. 2006. Cancer Res.66, 4368.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
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’.
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