5.30648

SIRT2 Inhibitor, AEM2

• Sinónimos: SIRT2 Inhibitor, AEM2, Sirtuin 2 Inhibitor
• Fórmula empírica (notación de Hill): C₂₇H₂₇N₃O
• Número de CAS: 1005095-04-4
• Peso molecular: 409.52
• UNSPSC Code: 12352200

Propiedades

• assay: ≥98% (HPLC)
• Quality Level: 100
• 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

Descripción

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
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

Información de seguridad

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable