TC-H 106

Modify Date: 2024-01-02 21:15:07

TC-H 106 Structure
TC-H 106 structure
Common Name TC-H 106
CAS Number 937039-45-7 Molecular Weight 339.431
Density 1.2±0.1 g/cm3 Boiling Point 627.3±45.0 °C at 760 mmHg
Molecular Formula C20H25N3O2 Melting Point N/A
MSDS Chinese USA Flash Point 333.1±28.7 °C

 Use of TC-H 106


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.

 Names

Name N'-(2-aminophenyl)-N-(4-methylphenyl)heptanediamide
Synonym More Synonyms

 TC-H 106 Biological Activity

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.
Related Catalog
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.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 627.3±45.0 °C at 760 mmHg
Molecular Formula C20H25N3O2
Molecular Weight 339.431
Flash Point 333.1±28.7 °C
Exact Mass 339.194672
PSA 84.22000
LogP 2.51
Appearance of Characters white solid
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.636
Storage condition -20℃

 Safety Information

RIDADR NONH for all modes of transport

 Articles2

More Articles
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).

Bioorg. Med. Chem. 23 , 5151-5, (2015)

Two of the histone deacetylases, TbDAC1 and TbDAC3, have been reported to be essential genes in trypanosomes. Therefore, we tested the activity of a panel of human histone deacetylase inhibitors (HDAC...

Inhibition of Histone Deacetylases Permits Lipopolysaccharide-Mediated Secretion of Bioactive IL-1β via a Caspase-1-Independent Mechanism.

J. Immunol. 195 , 5421-31, (2015)

Histone deacetylase (HDAC) inhibitors (HDACi) are clinically approved anticancer drugs that have important immune-modulatory properties. We report the surprising finding that HDACi promote LPS-induced...

 Synonyms

N-(2-Aminophenyl)-N'-(4-methylphenyl)heptanediamide
Pimelic Diphenylamide
Heptanediamide, N-(2-aminophenyl)-N-(4-methylphenyl)-
Pimelic Diphenylamide 106
TC-H 106