| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
TC-H 106 targets class I histone deacetylases (HDACs), specifically HDAC1, HDAC2, and HDAC3. HDACs are enzymes that remove acetyl groups from histone proteins, regulating gene expression. By inhibiting class I HDACs, TC-H 106 promotes histone acetylation and alters gene transcription. The compound is brain-penetrant and shows no activity against class II HDACs.
|
|---|---|
| ln Vitro |
In vitro, TC-H 106 is a slow, tight-binding inhibitor of class I HDACs with Ki values of 148 nM for HDAC1, about 102 nM for HDAC2, and 14 nM for HDAC3. It inhibits HDAC1, HDAC2, and HDAC3 with IC50 values of 150 nM, 760 nM, and 370 nM, respectively. The compound shows no activity against class II HDACs.
|
| ln Vivo |
In vivo, TC-H 106 is brain-penetrant and has been studied in models of neurological and psychiatric disorders where HDAC inhibition plays a role. By inhibiting class I HDACs in the brain, the compound modulates gene expression and has potential applications in the study of depression, schizophrenia, and neurodegenerative diseases.
|
| Enzyme Assay |
In vitro enzyme assays for TC-H 106 measure its inhibition of HDAC1, HDAC2, and HDAC3 activity. The enzyme is incubated with a fluorogenic substrate and varying concentrations of the compound. Deacetylase activity is measured by fluorescence, and IC50 or Ki values are calculated from dose-response curves. Selectivity over class II HDACs is confirmed by testing against class II enzymes.
|
| Cell Assay |
In vitro cell-based assays for TC-H 106 assess its effects on histone acetylation in cultured cells. Cells are treated with serial dilutions of the compound, and histone acetylation levels are measured by Western blotting using acetylation-specific antibodies. Gene expression changes are assessed by qPCR. Cell viability and proliferation are measured in parallel.
|
| Animal Protocol |
In vivo animal models for TC-H 106 include models of neurological and psychiatric disorders. The compound is administered via appropriate routes, and its effects on behavior, histone acetylation in brain tissues, and disease progression are evaluated. Pharmacodynamic studies measure HDAC inhibition and histone acetylation in target tissues.
|
| ADME/Pharmacokinetics |
TC-H 106 has a molecular formula of C20H25N3O2 and a molecular weight of 339.43 g/mol. It is also known as Pimelic Diphenylamide 106, RGFA-8, and Histone Deacetylase Inhibitor VII. The compound has a purity of ≥98%. It is soluble in DMSO and is stored at appropriate temperatures for research use.
|
| Toxicity/Toxicokinetics |
The toxicity profile of TC-H 106 is characterized in preclinical safety studies. As an HDAC inhibitor, the compound may affect gene expression and cellular differentiation. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
|
| References | |
| Additional Infomation |
N'-(2-aminophenyl)-N-(4-methylphenyl)heptadecamide is an aromatic amine and aromatic amide.
TC-H 106 (Pimelic Diphenylamide 106) is a slow, tight-binding inhibitor of class I histone deacetylases (HDACs) with Ki values of 148 nM for HDAC1, about 102 nM for HDAC2, and 14 nM for HDAC3. It is brain-penetrant and shows no activity against class II HDACs. TC-H 106 is also known as RGFA-8 and Histone Deacetylase Inhibitor VII. It is intended for laboratory research use only. |
| Molecular Formula |
C20H25N3O2
|
|---|---|
| Molecular Weight |
339.4314
|
| Exact Mass |
339.194
|
| Elemental Analysis |
C, 70.77; H, 7.42; N, 12.38; O, 9.43
|
| CAS # |
937039-45-7
|
| Related CAS # |
Pimelic Diphenylamide 106 (analog);2070015-24-4
|
| PubChem CID |
16070100
|
| Appearance |
White to yellow solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
627.3±45.0 °C at 760 mmHg
|
| Flash Point |
333.1±28.7 °C
|
| Vapour Pressure |
0.0±1.8 mmHg at 25°C
|
| Index of Refraction |
1.636
|
| LogP |
2.51
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
25
|
| Complexity |
419
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(CCCCCC(NC1C(N)=CC=CC=1)=O)NC1C=CC(C)=CC=1
|
| InChi Key |
WTKBRPXPNAKVEQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H25N3O2/c1-15-11-13-16(14-12-15)22-19(24)9-3-2-4-10-20(25)23-18-8-6-5-7-17(18)21/h5-8,11-14H,2-4,9-10,21H2,1H3,(H,22,24)(H,23,25)
|
| Chemical Name |
N'-(2-aminophenyl)-N-(4-methylphenyl)heptanediamide
|
| Synonyms |
TC-H 106, TC-H106, TC-H-106, TCH-106, TCH 106, TCH106, Histone Deacetylase Inhibitor VII, Pimelic Diphenylamide 106
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~368.26 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.55 mg/mL (1.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.55 mg/mL (1.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.55 mg/mL (1.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.