PTACH
Based on 1 Customer Validation
PTACH (NCH-51) is a potent HDAC inhibitor with IC50s of 48 nM, 32 nM, and 41 nM for HDAC1, HDAC4, and HDAC6, respectively. PTACH exerts potent growth inhibition against various cancer cells (EC50s of 1.1-9.1 μM) .
For research use only. We do not sell to patients.
- Purity: 97.04%
- CAS No.: 848354-66-5
- Formula: C20H26N2O2S2
- Molecular Weight:390.56
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
|
HDAC1 48 nM (IC50) |
HDAC4 32 nM (IC50) |
HDAC6 41 nM (IC50) |
HIV-1 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A498 | EC50 |
6.8 μM
Compound: NCH-51
|
Inhibition of A498 cell proliferation (mean)
Inhibition of A498 cell proliferation (mean)
|
[PMID: 17257837] |
| DLD-1 | EC50 |
2.3 μM
Compound: NCH-51
|
Inhibition of DLD-1 cell proliferation (mean)
Inhibition of DLD-1 cell proliferation (mean)
|
[PMID: 17257837] |
| DU-145 | EC50 |
4.5 μM
Compound: 51
|
Effective Concentration of compound to inhibit the growth of human DU-145 cells
Effective Concentration of compound to inhibit the growth of human DU-145 cells
|
[PMID: 15715470] |
| DU-145 | EC50 |
4.5 μM
Compound: 58
|
Inhibition of human DU145 cells
Inhibition of human DU145 cells
|
[PMID: 18247554] |
| HCT-116 | EC50 |
1.3 μM
Compound: NCH-51
|
Inhibition of HCT116 cell proliferation (mean)
Inhibition of HCT116 cell proliferation (mean)
|
[PMID: 17257837] |
| HCT-116 | EC50 |
3 μM
Compound: 51
|
Effective Concentration of compound to inhibit the growth of human HCT116 cells
Effective Concentration of compound to inhibit the growth of human HCT116 cells
|
[PMID: 15715470] |
| HCT-116 | EC50 |
3 μM
Compound: 58
|
Inhibition of human HCT116 cells
Inhibition of human HCT116 cells
|
[PMID: 18247554] |
| LOX IMVI | EC50 |
1.1 μM
Compound: 51
|
Effective Concentration of compound to inhibit the growth of human LOX-IMVI cells
Effective Concentration of compound to inhibit the growth of human LOX-IMVI cells
|
[PMID: 15715470] |
| LOX IMVI | EC50 |
1.1 μM
Compound: 58
|
Inhibition of human LOX-IMVI cells
Inhibition of human LOX-IMVI cells
|
[PMID: 18247554] |
| Malme-3M | EC50 |
4.3 μM
Compound: NCH-51
|
Inhibition of MALME-3M cell proliferation (mean)
Inhibition of MALME-3M cell proliferation (mean)
|
[PMID: 17257837] |
| MDA-MB-231 | EC50 |
2.3 μM
Compound: 51
|
Effective Concentration of compound to inhibit the growth of human MDA-MB-231 cells
Effective Concentration of compound to inhibit the growth of human MDA-MB-231 cells
|
[PMID: 15715470] |
| MDA-MB-231 | EC50 |
2.3 μM
Compound: 58
|
Inhibition of human MDA-MB-231 cells
Inhibition of human MDA-MB-231 cells
|
[PMID: 18247554] |
| MDA-MB-231 | EC50 |
4.4 μM
Compound: NCH-51
|
Inhibition of MDA-MB-231 cell proliferation (mean of two experiments)
Inhibition of MDA-MB-231 cell proliferation (mean of two experiments)
|
[PMID: 17257837] |
| NCI-H226 | EC50 |
2.6 μM
Compound: 51
|
Effective Concentration of compound to inhibit the growth of human NCI-H226 cells
Effective Concentration of compound to inhibit the growth of human NCI-H226 cells
|
[PMID: 15715470] |
| NCI-H226 | EC50 |
2.6 μM
Compound: 58
|
Inhibition of human NCI-H226 cells
Inhibition of human NCI-H226 cells
|
[PMID: 18247554] |
| NCI-H460 | EC50 |
2 μM
Compound: 58
|
Inhibition of human NCI-H460 cells
Inhibition of human NCI-H460 cells
|
[PMID: 18247554] |
| NCI-H460 | EC50 |
2.1 μM
Compound: 51
|
Inhibition of human lung cancer NCI-H460 cell growth
Inhibition of human lung cancer NCI-H460 cell growth
|
[PMID: 15715470] |
| NCI-H460 | EC50 |
2.1 μM
Compound: NCH-51
|
Inhibition of NCI-H460 cell proliferation (mean)
Inhibition of NCI-H460 cell proliferation (mean)
|
[PMID: 17257837] |
| PC-3 | EC50 |
9.5 μM
Compound: NCH-51
|
Inhibition of PC-3 cell proliferation (mean)
Inhibition of PC-3 cell proliferation (mean)
|
[PMID: 17257837] |
| SK-OV-3 | EC50 |
4.5 μM
Compound: 51
|
Effective Concentration of compound to inhibit the growth of human SK-OV-3 cells
Effective Concentration of compound to inhibit the growth of human SK-OV-3 cells
|
[PMID: 15715470] |
| SK-OV-3 | EC50 |
4.5 μM
Compound: 58
|
Inhibition of human SKOV3 cells
Inhibition of human SKOV3 cells
|
[PMID: 18247554] |
| SNB-78 | EC50 |
9.1 μM
Compound: 51
|
Effective Concentration of compound to inhibit the growth of human SNB-78 cells
Effective Concentration of compound to inhibit the growth of human SNB-78 cells
|
[PMID: 15715470] |
| SNB-78 | EC50 |
9.1 μM
Compound: 58
|
Inhibition of human SNB78 cells
Inhibition of human SNB78 cells
|
[PMID: 18247554] |
| St-4 | EC50 |
5 μM
Compound: 51
|
Effective Concentration of compound to inhibit the growth of human St-4 cells
Effective Concentration of compound to inhibit the growth of human St-4 cells
|
[PMID: 15715470] |
| St-4 | EC50 |
5 μM
Compound: 58
|
Inhibition of human St4 cells
Inhibition of human St4 cells
|
[PMID: 18247554] |
| T47D | EC50 |
8.3 μM
Compound: NCH-51
|
Inhibition of T-47D cell proliferation (mean of two experiments)
Inhibition of T-47D cell proliferation (mean of two experiments)
|
[PMID: 17257837] |
PTACH (compound 51) treatment elevates the levels of acetylated histone H4 and p21WAF1/CIP1 in a dose-dependent manner[1].
In cancer cell growth inhibition assay, PTACH (compound 51) shows strong activity. PTACH inhibits various cancer cells with EC50 values of 2.3 μM, 9.1 μM, 3.0 μM, 2.6 μM, 1.1 μM, 4.5 μM, 2.4 μM, 5.0 μM, and 4.5 μM for MDA-MB-231, SNB-78, HCT116, NCI-H226, LOX-IMVI, SK-OV-3, RXF-631L, St-4, and DU-145 cells, respectively[1].
PTACH (NCH-51) augments the HIV-1 production in latently infected OM10.1 cells and such reactivation is associated with a loss of HDAC1 occupancy and subsequent hyperacetylation of histones in nuc-1 at the HIV-1 promoter[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT 116 cells
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Concentration:1 μM, 5 μM, 25 μM
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Incubation Time:8 hours
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Result:Gave rise to elevated and dose-dependent levels of acetylated histone H4 and p21WAF1/CIP1.
Chemical Information
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CAS No. 848354-66-5
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Appearance Solid
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Molecular Weight 390.56
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Formula C20H26N2O2S2
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Color White to off-white
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SMILES
CC(C)C(SCCCCCCC(NC1=NC(C2=CC=CC=C2)=CS1)=O)=O
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Synonyms
NCH-51
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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
Solvent & Solubility
DMSO : 50 mg/mL (128.02 mM; Need ultrasonic; 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: ≥ 2.5 mg/mL (6.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (271 KB)
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SDS (476 KB)
- English - EN (476 KB)
- Français - FR (476 KB)
- Deutsch - DE (476 KB)
- Norwegian - NO (476 KB)
- Español - ES (476 KB)
- Swedish - SV (476 KB)
- Italian - IT (476 KB)
- Korean - KR (476 KB)
- Portuguese - PT (476 KB)
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Handling Instructions (2659 KB)
References
[1]. Suzuki T, et al. Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates. J Med Chem. 2005 Feb 24;48(4):1019-1032. [Content Brief]
[2]. Ann Florence B Victoriano, et al. Novel histone deacetylase inhibitor NCH-51 activates latent HIV-1 gene expression. FEBS Lett. 2011 Apr 6;585(7):1103-11. [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 | 2.5604 mL | 12.8021 mL | 25.6043 mL | 64.0107 mL |
| 5 mM | 0.5121 mL | 2.5604 mL | 5.1209 mL | 12.8021 mL | |
| 10 mM | 0.2560 mL | 1.2802 mL | 2.5604 mL | 6.4011 mL | |
| 15 mM | 0.1707 mL | 0.8535 mL | 1.7070 mL | 4.2674 mL | |
| 20 mM | 0.1280 mL | 0.6401 mL | 1.2802 mL | 3.2005 mL | |
| 25 mM | 0.1024 mL | 0.5121 mL | 1.0242 mL | 2.5604 mL | |
| 30 mM | 0.0853 mL | 0.4267 mL | 0.8535 mL | 2.1337 mL | |
| 40 mM | 0.0640 mL | 0.3201 mL | 0.6401 mL | 1.6003 mL | |
| 50 mM | 0.0512 mL | 0.2560 mL | 0.5121 mL | 1.2802 mL | |
| 60 mM | 0.0427 mL | 0.2134 mL | 0.4267 mL | 1.0668 mL | |
| 80 mM | 0.0320 mL | 0.1600 mL | 0.3201 mL | 0.8001 mL | |
| 100 mM | 0.0256 mL | 0.1280 mL | 0.2560 mL | 0.6401 mL |