382173

Histone Deacetylase Inhibitor VII, 106

The Histone Deacetylase Inhibitor VII, 106, also referenced under CAS 937039-45-7, controls the biological activity of Histone Deacetylase. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Synonim(y): Histone Deacetylase Inhibitor VII, 106, N¹-(2-Aminophenyl)-N⁷- p-tolylheptanediamide, Pimelic Diphenylamide 106
• Wzór empiryczny (zapis Hilla): C₂₀H₂₅N₃O₂
• Numer CAS: 937039-45-7
• Masa cząsteczkowa: 339.43
• Numer MDL: MFCD17010287
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white
• rozpuszczalność: DMSO: 10 mg/mL; ethanol: 2.5 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: −20°C
• InChI: 1S/C20H25N3O2/c1-15-11-13-16(14-12-15)22-19(24)9-3-2-4-10-20(25)23-18-8-6-5-7-17(18)21/h5-8,11-14H,2-4,9-10,21H2,1H3,(H,22,24)(H,23,25)
• Klucz InChI: WTKBRPXPNAKVEQ-UHFFFAOYSA-N

Opis

Opis ogólny

A cell-permeable p-tolylbenzamide and a Histone Deacetylase (HDAC) Inhibitor IV (Cat. No. 382170) analog that acts as a selective inhibitor against class I HDAC1,2,3 (IC₅₀ = 0.15, 0.76, and 0.37 µM with 15, 30, and 180 min preincubation, respectively), while exhibiting much lower acitivity against class I HDAC8 (IC₅₀ ≥ 5µM with 3 h preincubation) and no activity against class II HDAC4/5/7 even at concentrations as high as 180µM. Although the mode of inhibition is mechanistically competitive and reversible, due to the slow- and tight-binding nature, long preincubation is often required for effective in vitro enzyme inhibition, while 106-induced cellular H3 hyperacetylation is shown to persist for more than 6 hours after inhibitor removal by washing in GM15850 culture. 106 is reported to be less cytotoxic than TSA (Cat. No. 647925), MS-275, and SAHA (EC₅₀ = 6.3, 0.328, 0.768, and 1.5 µM, respectively, in GM15850 killing).

A cell-permeable p-tolylbenzamide and a Histone Deacetylase (HDAC) Inhibitor IV (Cat. No. 382170) analog that acts as a selective inhibitor against class I HDAC1/2/3 (IC₅₀ = 0.15/0.76/0.37 µM with 15/30/180 min preincubation), while exhibiting much lower acitivity against class I HDAC8 (IC₅₀ ≥ 5µM with 3 h preincubation) and no activity against class II HDAC4/5/7 even at concentrations as high as 180µM. Although the mode of inhibition is mechanistically competitive and reversible, due to the slow- and tight-binding nature, long preincubation is often required for effective in vitro enzyme inhibition, while 106-induced cellular H3 hyperacetylation is shown to persist for more than 6 hours after inhibitor removal by washing in GM15850 culture. 106 is reported to be less cytotoxic than TSA (Cat. No. 647925), MS-275, and SAHA (EC₅₀ = 6.3, 0.328, 0.768, and 1.5 µM, respectively, in GM15850 killing).

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

Chou, C.J., et al. 2008. J. Biol. Chem.283, 35402.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable