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382173  Histone Deacetylase Inhibitor VII, 106

N¹-(2-Aminophenyl)-N7-p-tolylheptanediamide, Pimelic Diphenylamide 106

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07 February 2012

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382173-5MG  5 mg 
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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).
Product information
Form Yellow solid
Molar mass 339.4
Protect from Light Yes
Packaged under inert gas Yes
Purity ≥95% by HPLC
Solubility DMSO or EtOH
Chemical formula C20H25N3O2
CAS number 937039-45-7
Store and ship information
Storage -20°C
Ship Ambient Temperature Only
Standard Handling
Safety information
S Phrase S: 22-24/25-36

Do not breathe dust.
Avoid contact with skin and eyes.
Wear suitable protective clothing.
Histone Deacetylase Inhibitor VII, 106, molecular structure

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© Merck KGaA, Darmstadt, Germany, 2012

All references to Merck refer to Merck KGaA, Darmstadt, Germany.

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