Pimelic Diphenylamide 106
Based on 5 publication(s) in Google Scholar
Pimelic Diphenylamide 106 (TC-H 106) is a slow, tight binding class I HDAC inhibitor (inhibits HDAC1, 2, and 3 with IC50 values of 150 nM, 760 nM, and 370 nM, respectively), with no activity against class II HDACs. Pimelic Diphenylamide 106 modulates dopamine concentration and protects dopamine cells by inducing VMAT2 expression. Pimelic Diphenylamide 106 can be used in the study of neuropsychiatric diseases such as attention deficit hyperactivity disorder (ADHD).
For research use only. We do not sell to patients.
- Purity: 98.54%
- CAS No.: 937039-45-7
- Formula: C20H25N3O2
- Molecular Weight:339.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Pimelic Diphenylamide 106
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Biological Activity
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HDAC1 150 nM (IC50) |
HDAC3 370 nM (IC50) |
HDAC2 760 nM (IC50) |
HDAC8 5000 nM (IC50) |
Pimelic Diphenylamide 106 (0-10 μM; 24 h) reduces the damage and cell death of SH-SY5Y cells induced by 6-OHDA (500 μM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y cell line
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Concentration:0, 0.1, 1 and 10 µM
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Incubation Time:24 h
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Result:Induced VMAT2 gene expression.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pups born to mothers injected with corticosterone showed hyperactive behavior and cognitive impairment[3]
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Dosage:50 mg/kg
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Administration:i.p.; Start on the 18th to 20th day after birth, once a day for 3 days
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Result:Increased VMAT2 expression in mouse brain.
Chemical Information
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CAS No. 937039-45-7
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Appearance Solid
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Molecular Weight 339.43
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Formula C20H25N3O2
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Color White to yellow
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SMILES
O=C(NC1=CC=CC=C1N)CCCCCC(NC2=CC=C(C)C=C2)=O
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Synonyms
RGFA-8; TC-H 106; Histone Deacetylase Inhibitor VII
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Fusobacterium nucleatum facilitates anti-PD-1 therapy in microsatellite stable colorectal cancer. [Abstract]2024 Oct 14;42(10):1729-1746.e8. PMID: 39303724 -
Cell Metab
Microbial regulation of hexokinase 2 links mitochondrial metabolism and cell death in colitis. [Abstract]2021 Dec 7;33(12):2355-2366.e8. PMID: 34847376 -
Adv Sci (Weinh)
The Probiotic Parabacteroides johnsonii Ameliorates Metabolic Disorders Through Promoting BCAAs to BSCFAs Conversion. [Abstract]2025 Aug 7:e02624. PMID: 40772426 -
JCI Insight
Transcriptional control of a collagen deposition and adhesion process that promotes lung adenocarcinoma growth and metastasis. [Abstract]2022 Jan 11;7(1):e153948. PMID: 34874914 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471
Solvent & Solubility
DMSO : 125 mg/mL (368.26 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.55 mg/mL (1.62 mM); Clear solution
This protocol yields a clear solution of ≥ 0.55 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.55 mg/mL (1.62 mM); Clear solution
This protocol yields a clear solution of ≥ 0.55 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[3]. Lee, et al. "Dopaminergic cell protection and alleviation of neuropsychiatric disease symptoms by VMAT2 expression through the class I HDAC inhibitor TC‐H 106." Pharmacology Research & Perspectives 11.5 (2023): e01135. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9461 mL | 14.7306 mL | 29.4612 mL | 73.6529 mL |
| 5 mM | 0.5892 mL | 2.9461 mL | 5.8922 mL | 14.7306 mL | |
| 10 mM | 0.2946 mL | 1.4731 mL | 2.9461 mL | 7.3653 mL | |
| 15 mM | 0.1964 mL | 0.9820 mL | 1.9641 mL | 4.9102 mL | |
| 20 mM | 0.1473 mL | 0.7365 mL | 1.4731 mL | 3.6826 mL | |
| 25 mM | 0.1178 mL | 0.5892 mL | 1.1784 mL | 2.9461 mL | |
| 30 mM | 0.0982 mL | 0.4910 mL | 0.9820 mL | 2.4551 mL | |
| 40 mM | 0.0737 mL | 0.3683 mL | 0.7365 mL | 1.8413 mL | |
| 50 mM | 0.0589 mL | 0.2946 mL | 0.5892 mL | 1.4731 mL | |
| 60 mM | 0.0491 mL | 0.2455 mL | 0.4910 mL | 1.2275 mL | |
| 80 mM | 0.0368 mL | 0.1841 mL | 0.3683 mL | 0.9207 mL | |
| 100 mM | 0.0295 mL | 0.1473 mL | 0.2946 mL | 0.7365 mL |