[1]. Chou CJ, et al. Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases. J Biol Chem. 2008 Dec 19;283(51):35402-35409.
[2]. Xu C, et al. Chemical probes identify a role for histone deacetylase 3 in Friedreich’s ataxia gene silencing. Chem Biol. 2009 Sep 25;16(9):980-989.
[1]. Chou CJ, et al. Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases. J Biol Chem. 2008 Dec 19;283(51):35402-35409.
[2]. Xu C, et al. Chemical probes identify a role for histone deacetylase 3 in Friedreich’s ataxia gene silencing. Chem Biol. 2009 Sep 25;16(9):980-989.
[1]. Chou CJ, et al. Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases. J Biol Chem. 2008 Dec 19;283(51):35402-35409.
[2]. Xu C, et al. Chemical probes identify a role for histone deacetylase 3 in Friedreich’s ataxia gene silencing. Chem Biol. 2009 Sep 25;16(9):980-989.
Pimelic Diphenylamide 106 is a slow, tight-binding inhibitor of class I HDAC (HDAC 1, 2, and 3, with IC50 values of 150 nM , 760nM, and 370 nM, respectively), demonstrating no activity against class II HDACs. IC50 value: 150 nM (HDAC1), 370 nM (HDAC3), 760nM(HDAC2) Target: HDAC in vitro: Pimelic Diphenylamide 106 has preference toward HDAC3 with Ki of 14 nM, 15 times lower than the Ki for HDAC1. Pimelic Diphenylamide 106 exhibits weaker inhibitory activities against HDAC 8 with IC50 of 5 μM after a 3-h preincubation with HDAC8.
IC50 & Target
HDAC1
150 nM (IC50)
HDAC3
370 nM (IC50)
HDAC2
760 nM (IC50)
HDAC8
5000 nM (IC50)
分子量
339.43
Formula
C20H25N3O2
CAS 号
937039-45-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 125 mg/mL (368.26 mM; ultrasonic and warming and heat to 60°C)
[1]. Chou CJ, et al. Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases. J Biol Chem. 2008 Dec 19;283(51):35402-35409.
[2]. Xu C, et al. Chemical probes identify a role for histone deacetylase 3 in Friedreich’s ataxia gene silencing. Chem Biol. 2009 Sep 25;16(9):980-989.