1440209-96-0

Basic information

• Product Name: BRD73954
• Synonyms: BRD73954;N1-hydroxy-N3-phenethylisophthalamide;N1-hydroxy-N3-(2-phenylethyl)-1,3-benzenedicarboxamide BRD73954;N1-Hydroxy-N3-(2-phenylethyl)-1,3-benzenedicarboxamide;BRD73954, 1-N-hydroxy-3-N-(2-phenylethyl)benzene-1,3-dicarboxamide
• CAS NO: 1440209-96-0
• Molecular Formula: C16H16N2O3
• Molecular Weight: 284.30984
• EINECS: -0
• Product Categories: Inhibitors
• Mol File: 1440209-96-0.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• Density: 1.245±0.06 g/cm3(Predicted)
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• Solubility: DMSO (Slightly), Methanol (Slightly)
• PKA: 8.56±0.10(Predicted)
• CAS DataBase Reference: BRD73954(CAS DataBase Reference)
• NIST Chemistry Reference: BRD73954(1440209-96-0)
• EPA Substance Registry System: BRD73954(1440209-96-0)

Safety Data

• Hazardous Substances Data: 1440209-96-0(Hazardous Substances Data)

Usage

Description

BRD73954 is a dual inhibitor of histone deacetylase 6 (HDAC6) and HDAC8, selectively targeting these enzymes over HDAC1-5, -7, and -9. With IC50s of 36 and 120 nM for HDAC6 and HDAC8, respectively, BRD73954 increases the acetylation of α-tubulin, a known HDAC6 substrate, without affecting histone H3, a substrate for HDAC1, -2, and -3. This small molecule inhibitor plays a role in affecting cell adhesion and mobility in cells.

Uses

Used in Pharmaceutical Industry:
BRD73954 is used as a therapeutic agent for targeting HDAC6 and HDAC8, which are involved in various cellular processes. Its selective inhibition of these histone deacetylases can potentially lead to the development of treatments for diseases where HDAC6 and HDAC8 play a significant role.
Used in Research Applications:
In the field of biological and medical research, BRD73954 serves as a valuable tool for studying the functions and roles of HDAC6 and HDAC8 in cellular processes. By inhibiting these specific enzymes, researchers can gain insights into their contributions to cell adhesion, mobility, and other related cellular functions.
Used in Drug Development:
BRD73954's ability to inhibit HDAC6 and HDAC8 makes it a promising candidate for the development of new drugs targeting these enzymes. Its selective inhibition can be leveraged to design drugs with fewer side effects and higher efficacy in treating diseases associated with the dysregulation of HDAC6 and HDAC8.

references

[1]. olson de, wagner ff, kaya t, et al. discovery of the first histone deacetylase 6/8 dual inhibitors. j med chem, 2013, 56(11): 4816-4820.

Upstream product

• 925159-24-6 C₁₇H₁₇NO₃ 
• 1877-71-0 benzene 1,3-dicarboxylic acid monomethyl ester 
• 64-04-0 phenethylamine 

Relevant articles and documents

Discovery of the first histone deacetylase 6/8 dual inhibitors

We disclose the first small molecule histone deacetylase (HDAC) inhibitor (3, BRD73954) capable of potently and selectively inhibiting both HDAC6 and HDAC8 despite the fact that these isoforms belong to distinct phylogenetic classes within the HDAC family of enzymes. Our data demonstrate that meta substituents of phenyl hydroxamic acids are readily accommodated upon binding to HDAC6 and, furthermore, are necessary for the potent inhibition of HDAC8.