5.30648

SIRT2 Inhibitor, AEM2

• Sinonimo/i: SIRT2 Inhibitor, AEM2, Sirtuin 2 Inhibitor
• Formula empirica (notazione di Hill): C₂₇H₂₇N₃O
• Numero CAS: 1005095-04-4
• Peso molecolare: 409.52
• Codice UNSPSC: 12352200

Proprietà

• Saggio: ≥98% (HPLC)
• Livello qualitativo: 100
• Stato: solid
• Potenza: 3.8 μM IC₅₀
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: white
• Solubilità: DMSO: 50 mg/mL
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
SIRT2

Reversible: yes

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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.

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable