5.30648

SIRT2 Inhibitor, AEM2

• 別名: SIRT2 Inhibitor, AEM2, Sirtuin 2 Inhibitor
• 実験式（ヒル表記法）: C₂₇H₂₇N₃O
• CAS番号: 1005095-04-4
• 分子量: 409.52
• UNSPSCコード: 12352200

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: solid
• 有効性: 3.8 μM IC₅₀
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 50 mg/mL
• 保管温度: 2-8°C

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
SIRT2

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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.

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable