Cas No.: | 937039-45-7 |
Synonyms: | RGFA-8; TC-H 106; Histone Deacetylase Inhibitor VII |
SMILES: | C(NC1=CC=CC=C1N)(=O)CCCCCC(NC1=CC=C(C)C=C1)=O |
Formula: | C20H25N3O2 |
M.Wt: | 339.43 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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. |
Target: | HDAC1:150 nM (IC50) HDAC3:370 nM (IC50) HDAC2:760 nM (IC50) HDAC8:5000 nM (IC50) |
References: | [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. |