All Photos(1)
Synonym(s):
SIRT2 Inhibitor, AEM2, Sirtuin 2 Inhibitor
Empirical Formula (Hill Notation):
C27H27N3O
Recommended Products
Assay
≥98% (HPLC)
Quality Level
form
solid
potency
3.8 μM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
A cell permeable methanophenanthridine derivative that acts a selective inhibitor of SIRT2 (IC50 = 3.8 µM) and exhibits ~30 fold greater selectivity over SIRT1 (IC50 >100 µM) and SIRT3. Blocks SIRT2-induced p53 deacetylation and thereby elevates p53 levels and causes increased expression of CDKN1A, PUMA, and NOXA in non-small cell lung cancer (NSCLC) A549 cells. Also shown to reduce NSCLC cell viability by 50% (~20 µM) and inhibit their proliferation. Sensitizes A549 cancer cell line to etoposide (~1 µM) induced DNA damage in a p53-dependent manner.
A cell permeable methanophenanthridine derivative that acts a selective inhibitor of SIRT2 (IC50 = 3.8 µM) and exhibits ~30 fold greater selectivity over SIRT1 (IC50 >100 µM) and SIRT3. Blocks SIRT2-induced p53 deacetylation and thereby elevates p53 levels and causes increased expression of CDKN1A, PUMA, and NOXA in non-small cell lung cancer (NSCLC) A549 cells. Also shown to reduce NSCLC cell viability by 50% (~20 µM) and inhibit their proliferation. Sensitizes A549 cancer cell line to etoposide (~1 µM) induced DNA damage in a p53-dependent manner.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
SIRT2
SIRT2
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 1 month at -70°C.
Use only fresh DMSO for reconstitution.
Other Notes
Hoffmann G., et al. 2014. J. Biol. Chem.289, 5208.
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
Regulatory Information
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Certificates of Analysis (COA)
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Gesine Hoffmann et al.
The Journal of biological chemistry, 289(8), 5208-5216 (2014-01-01)
Sirtuin 2 (SIRT2) is an NAD(+)-dependent protein deacetylase whose targets include histone H4 lysine 16, p53, and α-tubulin. Because deacetylation of p53 regulates its effect on apoptosis, pharmacological inhibition of SIRT2-dependent p53 deacetylation is of great therapeutic interest for the
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