251635

Daminozide

• Synonim(y): Inhibitor XII demetylazy lizyny histonowej, Inhibitor VI LSD1, kwas N,N-dimetyloaminobursztynamowy, kwas bursztynowy-2,2-dimetylohydrazyd, kwas 4-(2,2-dimetylohydrazynylo)-4-oksobutanowy, Inhibitor VI BHC100, Inhibitor VI KDM2A, Inhibitor VI KIAA1718, Inhibitor VI LSD, Inhibitor VI PHF8, Inhibitor VI JHDM
• Wzór empiryczny (zapis Hilla): C₆H₁₂N₂O₃
• Numer CAS: 1596-84-5
• Masa cząsteczkowa: 160.17
• Numer MDL: MFCD00002787
• Kod UNSPSC: 12352200

Właściwości

• Próba: ≥98% (NMR)
• Poziom jakości: 100
• Formularz: powder
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated (hygroscopic); protect from light
• kolor: white
• rozpuszczalność: water: 10 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 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)
• Klucz InChI: NOQGZXFMHARMLW-UHFFFAOYSA-N

Opis

Opis ogólny

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.

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Harmful & Carcinogenic / Teratogenic (E)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Piktogramy: GHS08
• Hasło ostrzegawcze: Warning
• Zwroty wskazujące rodzaj zagrożenia: H351
• Zwroty wskazujące środki ostrożności: P201 - P202 - P280 - P308 + P313 - P405 - P501
• Klasyfikacja zagrożeń: Carc. 2
• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 2
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable