Pimelic Diphenylamide 106(TC-H 106)

  Cat. No.:  DC8661   Featured
Chemical Structure
937039-45-7
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Field of application
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.
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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