A slow

Pimelic Diphenylamide 106 – 25 mg

Brand:
Cayman
CAS:
937039-45-7
Storage:
-20
UN-No:
Non-Hazardous - /

Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases (HDACs).{16844} Unlike the HDAC inhibitor suberoylanilide hydroamic acid, which has a fast-on/fast-off HDAC binding rate, pimelic diphenylamide 106 progressively binds HDACs and remains bound after wash-out. As a result, the IC50 of pimelic diphenylamide 106 decreases over time. With prolonged preincubation (1-3 hours), pimelic diphenylamide inhibits the class I HDACs (IC50 = 150, 760, 370, and 5,000 nM for HDAC1, 2, 3, and 8, respectively) but not the class II HDACs (IC50 > 180 μM for HDAC4, 5, and 7).{16844} Pimelic diphenylamide 106 and related benzamide HDAC inhibitors may have therapeutic value in Friedrich’s ataxia{16844,17391,17392} and Huntington’s disease,{17390} in part due to their low animal toxicity.  

 

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Description

A slow, tight-binding inhibitor of class I HDACs, progressively binding HDACs and remaining bound after wash-out; inhibits class I HDACs (IC50 = 150, 760, 370, and 5,000 nM for HDAC1, 2, 3, and 8, respectively) but not class II HDACs (IC50 > 180 µM for HDAC4, 5, and 7)

Formal name: N1-(2-aminophenyl)-N7-(4-methylphenyl)-heptanediamide

Synonyms:  Histone Deacetylase Inhibitor VII|TC-H 106

Molecular weight: 339.4

CAS: 937039-45-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Deacetylases||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Deacetylation

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