SIRT2 Inhibitor, AEM2

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.

Cell permeable: yes

Primary Target
SIRT2

Reversible: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

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.

Hoffmann G., et al. 2014. J. Biol. Chem.289, 5208.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany