5.30648

SIRT2 Inhibitor, AEM2

• Synonym(e): SIRT2 Inhibitor, AEM2, Sirtuin 2 Inhibitor
• Empirische Formel (Hill-System): C₂₇H₂₇N₃O
• CAS-Nummer: 1005095-04-4
• Molekulargewicht: 409.52
• UNSPSC-Code: 12352200

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Wirksamkeit: 3.8 μM IC₅₀
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: white
• Löslichkeit: DMSO: 50 mg/mL
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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. Wirkung

Cell permeable: yes

Primary Target
SIRT2

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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.

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable