251635

Daminozide

• Sinonimo/i: 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
• Formula empirica (notazione di Hill): C₆H₁₂N₂O₃
• Numero CAS: 1596-84-5
• Peso molecolare: 160.17
• Numero MDL: MFCD00002787
• Codice UNSPSC: 12352200

Proprietà

• Saggio: ≥98% (NMR)
• Livello qualitativo: 100
• Forma fisica: powder
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic); protect from light
• Colore: white
• Solubilità: water: 10 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 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); NOQGZXFMHARMLW-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Harmful & Carcinogenic / Teratogenic (E)

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Pittogrammi: GHS08
• Avvertenze: Warning
• Indicazioni di pericolo: H351
• Consigli di prudenza: P201 - P202 - P280 - P308 + P313 - P405 - P501
• Classi di pericolo: Carc. 2
• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 2
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable