TC-H 106 (Synonyms: RGFA-8; TC-H 106; Histone Deacetylase Inhibitor VII) |
| Catalog No.GC13591 |
A tight-binding inhibitor of class I HDACs
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 937039-45-7
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 937039-45-7 | SDF | |
| Synonyms | RGFA-8; TC-H 106; Histone Deacetylase Inhibitor VII | ||
| Chemical Name | N'-(2-aminophenyl)-N-(4-methylphenyl)heptanediamide | ||
| Canonical SMILES | CC1=CC=C(C=C1)NC(=O)CCCCCC(=O)NC2=CC=CC=C2N | ||
| Formula | C20H25N3O2 | M.Wt | 339.43 |
| Solubility | ≥ 15.2mg/mL in DMSO, ≥ 7.46 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9461 mL | 14.7306 mL | 29.4612 mL |
| 5 mM | 0.5892 mL | 2.9461 mL | 5.8922 mL |
| 10 mM | 0.2946 mL | 1.4731 mL | 2.9461 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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