251635

Daminozide

• Sinônimo(s): 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
• Fórmula empírica (Notação de Hill): C₆H₁₂N₂O₃
• Número CAS: 1596-84-5
• Peso molecular: 160.17
• Número MDL: MFCD00002787
• Código UNSPSC: 12352200

Propriedades

• Ensaio: ≥98% (NMR)
• Nível de qualidade: 100
• Formulário: powder
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated (hygroscopic); protect from light
• cor: white
• solubilidade: water: 10 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 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)
• chave InChI: NOQGZXFMHARMLW-UHFFFAOYSA-N

Descrição

Descrição geral

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.

Embalagem

Packaged under inert gas

Advertência

Toxicity: Harmful & Carcinogenic / Teratogenic (E)

Reconstituição

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

Outras notas

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

Informações legais

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

Informações de segurança

• Pictogramas: GHS08
• Palavra indicadora: Warning
• Frases de perigo: H351
• Declarações de precaução: P201 - P202 - P280 - P308 + P313 - P405 - P501
• Classificações de perigo: Carc. 2
• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 2
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable