251635

Daminozide

• 別名: Daminozide, Histone Lysine Demethylase Inhibitor XII, LSD1 Inhibitor VI, N,N-Dimethylamino-succinamic acid, Succinic acid-2,2-dimethylhydrazide, 4-(2,2-Dimethylhydrazinyl)-4-oxobutanoic acid, BHC100 Inhibitor VI, KDM2A Inhibitor, KIAA1718 Inhibitor VI, LSD Inhibitor VI, PHF8 Inhibitor, JHDM Inhibitor VI
• 実験式（ヒル表記法）: C₆H₁₂N₂O₃
• CAS番号: 1596-84-5
• 分子量: 160.17
• MDL番号: MFCD00002787
• UNSPSCコード: 12352200

特性

• アッセイ: ≥98% (NMR)
• 品質水準: 100
• 形状: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 色: white
• 溶解性: water: 10 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• InChI: 1S/C6H12N2O3/c1-8(2)7-5(9)3-4-6(10)11/h3-4H2,1-2H3,(H,7,9)(H,10,11)
• InChI Key: NOQGZXFMHARMLW-UHFFFAOYSA-N

詳細

詳細

A dimethylamino substituted succinamate that, in addition to its well known use as a plant growth regulator, also acts as an inhibitor against histone lysine demthylases KDM2A, LSD1 (KDM7A; KIAA1718), and PHF8 (IC₅₀ = 1.5, 2.1, and 0.55 µM, respectively), but not KDM3A, KDM4E, KDM5C, KDM6B, or three hydroxylases (IC₅₀ >100 µM). Substrate-competition and/or active site Iron chelating likely accounts for the inhibitory activity against the FAD-dependent LSD1, while 2-oxoglutarate (2-OG) competition (K_i = 1.97 µM) appears as the major mode of action against KDM2A.

A dimethylamino substituted succinamic acid compound that, in addition to its well known use as a plant growth regulator, also acts as an inhibitor against histone lysine demthylases KDM2A, LSD1 (KDM7A; KIAA1718), and PHF8 (IC₅₀ = 1.5, 2.1, and 0.55 µM, respectively), but not KDM3A, KDM4E, KDM5C, KDM6B, (IC₅₀ >100 µM) or three hydroxylases (FIH, PHD2, and BBOX1; IC₅₀ >100 µM). Although kinetic studies indicate 2-oxoglutarate (2-OG) competition (K_i = 1.97 µM) as the major mode of action against KDM2A, substrate-competition and/or active site Iron chelation more likely accounts for the compound′s inhibitory activity against the FAD-dependent LSD1.

包装

Packaged under inert gas

警告

Toxicity: Harmful & Carcinogenic / Teratogenic (E)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

その他情報

Rose, N.R., et al. 2012. J. Med. Chem.55, 6639.

法的情報

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

安全性情報

• ピクトグラム: GHS08
• シグナルワード: Warning
• 危険有害性情報: H351
• 注意書き: P201 - P202 - P280 - P308 + P313 - P405 - P501
• 危険有害性の分類: Carc. 2
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable