首页 蛋白库 基因库 产品 会员服务
位置：首页 > 产品库 > TC-H 106
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
TC-H 106
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。
TC-H 106图片
CAS NO:937039-45-7

TC-H 106 是一种缓慢、紧密结合的 I 类 HDAC（HDAC 1、2 和 3，IC50 值分别为 150 nM、760nM 和 370 nM）抑制剂，对 II 类 HDAC 没有活性。
Cas No.937039-45-7
别名RGFA-8; TC-H 106; Histone Deacetylase Inhibitor VII
化学名N'-(2-aminophenyl)-N-(4-methylphenyl)heptanediamide
Canonical SMILESCC1=CC=C(C=C1)NC(=O)CCCCCC(=O)NC2=CC=CC=C2N
分子式C20H25N3O2
分子量339.43
溶解度≥ 15.2mg/mL in DMSO, ≥ 7.46 mg/mL in EtOH with ultrasonic
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

TC-H 106 is an inhibitor of Class I Histone Deacetylase with IC50 values of 150, 760, 370 and 5000 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively [1].

Histone deacetylases (HADC) 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. Class I histone deacetylase are consist of HDAC1, 2, 3 and 8 [1].

In a lymphoblastoid cell line from a Friedreich ataxia patient, TC-H 106 (2 μM) prolonged acetylation of histone H3 [1]. In HeLa cell, TC-H 106 inhibited HDACs with IC50 value of 1.3 μM. TC-H 106 inhibited recombinant HDAC3/NcoR2 and recombinant HDAC1 with IC50 values of 0.79 and 0.24 μM, respectively [2].

In KIKI mice carrying a (GAA) 230 repeats in the first intron of the mouse frataxin gene, TC-H 106 increased the level of frataxin mRNA. The histone H3 and H4 acetylation in chromatin near the GAA repeat was also increased. These results resulted in the frataxin return to the normal level in the nervous system and heart in KIKI mice [3].

References:
[1].  Chou CJ, Herman D, Gottesfeld JM. Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases. J Biol Chem, 2008, 283(51): 35402-35409.
[2].  Xu C, Soragni E, Chou CJ, et al. Chemical probes identify a role for histone deacetylase 3 in Friedreich's ataxia gene silencing. Chem Biol, 2009, 16(9): 980-989.
[3].  Rai M, Soragni E, Jenssen K, et al. HDAC inhibitors correct frataxin deficiency in a Friedreich ataxia mouse model. PLoS One, 2008, 3(4): e1958.

 
 
维奥蛋白资源库 - 中文蛋白资源 CopyRight © 2010-2024