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BRD73954
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
BRD73954图片
CAS NO:1440209-96-0
包装与价格：
包装价格(元)
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BRD73954 是一种有效的 HDAC 抑制剂，选择性地抑制 HDAC6 和 HDAC8，对 HDAC6、HDAC8、HDAC2、HDAC1 和 HDAC3 的 IC50 值分别为 0.0036、0.12、9、12、23 μM。 BRD73954 降低与 Ac-Tubulin 上调相关的 HDAC6 水平。
Cas No.1440209-96-0
化学名N1-hydroxy-N3-phenethylisophthalamide
Canonical SMILESONC(C1=CC=CC(C(NCCC2=CC=CC=C2)=O)=C1)=O
分子式C16H16N2O3
分子量284.31
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 1 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BRD73954 is a potent and selective inhibitor of HDAC with IC50 values of 36 and 120 nM for HDAC6 and HDAC8, respectively [1].

Histone deacetylases (HADCs) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription [1].

BRD73954 is a potent and selective HDAC inhibitor with IC50 values of 36 and 120 nM for HDAC6 and HDAC8, respectively. Also, BRD73954 inhibited HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC7 and HDAC9 with IC50 values of 12, 9.0, 23, >33, >33, 13 and >33 μM, respectively. In HeLa cells, BRD73954 significantly increased α-tubulin acetylation, which was a substrate for HDAC6, while there was no change in the acetylation state of histone H3, which was a substrate for HDACs 1, 2 and 3 [1].

Reference:
[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.

 
 
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