CPTH2
Based on 1 publication(s) in Google Scholar
CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B).
For research use only. We do not sell to patients.
- Purity: 99.82%
- CAS No.: 357649-93-5
- Formula: C14H14ClN3S
- Molecular Weight:291.80
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Histone Modification Research Compound Library
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Publications Citing Use of MedChemExpress (MCE) CPTH2
More
Biological Activity
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GCN5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BTI-TN-5B1-4 | IC50 |
262 nM
Compound: 2
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Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
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[PMID: 20579890] |
| BTI-TN-5B1-4 | IC50 |
7160 nM
Compound: 2
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Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
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[PMID: 20579890] |
CPTH2 (100 μM; 12, 24, 48 hours) causes a decrease in cell proliferation after as early as 12 h with a further significant reduction after 48 h stimulation[1].
CPTH2 (100 μM; 12 or 48 hours) causes a comparable drop of the activity in both cell lines[1].
CPTH2 (100 μM; 48 hours) produces a drastic increase in apoptotic/dead cell population after 48 h[1].
CPTH2 (100 μM; 12, 24, 48 hours) shows a reduced acetylation of both global AcH3 histone and H3AcK18[1].
CPTH2 (100 μM; 24, 48 hours) is capable to counteract invasion and migration of ccRCC-786-O cells in culture[1].
CPTH2 (0.2, 0.5, 1 mM) inhibits the growth of a GCN5 deleted strain and a single catalytic mutant E173H[2].
CPTH2 (0.6, 0.8 mM; for 24 hours) inhibits histone H3 acetylation in yeast cell cultures[2].
CPTH2 inhibits the Gcn5p dependent functional network[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Papillary thyroid (K1) and clear cell Renal Cell Carcinoma (ccRCC-786-O) cell lines
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Concentration:100 μM
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Incubation Time:12, 24, 48 hours
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Result:Caused a decrease in cell proliferation after as early as 12 h with a further significant reduction after 48 h stimulation.
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Cell Line:K1 and ccRCC-786-O cell lines
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Concentration:100 μM
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Incubation Time:24 hours (K1 cell) and 48 hours (ccRCC-786-O cell)
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Result:Caused a comparable drop of the activity in both cell lines.
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Cell Line:ccRCC-786-O cells
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Concentration:100 μM
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Incubation Time:48 hours
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Result:Produced a drastic increase in apoptotic/dead cell population after 48 h.
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Cell Line:ccRCC-786-O cells
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Concentration:100 μM
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Incubation Time:12, 24, 48 hours
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Result:Showed a reduced acetylation of both global AcH3 histone and H3AcK18.
Chemical Information
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CAS No. 357649-93-5
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Appearance Solid
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Molecular Weight 291.80
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Formula C14H14ClN3S
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Color White to yellow
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SMILES
ClC1=CC=C(C2=CSC(N/N=C3CCCC/3)=N2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 16.67 mg/mL (57.13 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)
Ethanol : 1 mg/mL (3.43 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 1.67 mg/mL (5.72 mM); Suspended solution
This protocol yields a suspended solution of ≥ 1.67 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Cocco E, et al. KAT3B-p300 and H3AcK18/H3AcK14 levels are prognostic markers for kidney ccRCC tumoraggressiveness and target of KAT inhibitor CPTH2. Clin Epigenetics. 2018 Apr 4;10:44. [Content Brief]
[2]. Chimenti F, et al. A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl)hydrazone. J Med Chem. 2009 Jan 22;52(2):530-6. [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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 3.4270 mL | 17.1350 mL | 34.2700 mL | 85.6751 mL |
| DMSO | 5 mM | 0.6854 mL | 3.4270 mL | 6.8540 mL | 17.1350 mL |
| 10 mM | 0.3427 mL | 1.7135 mL | 3.4270 mL | 8.5675 mL | |
| 15 mM | 0.2285 mL | 1.1423 mL | 2.2847 mL | 5.7117 mL | |
| 20 mM | 0.1714 mL | 0.8568 mL | 1.7135 mL | 4.2838 mL | |
| 25 mM | 0.1371 mL | 0.6854 mL | 1.3708 mL | 3.4270 mL | |
| 30 mM | 0.1142 mL | 0.5712 mL | 1.1423 mL | 2.8558 mL | |
| 40 mM | 0.0857 mL | 0.4284 mL | 0.8568 mL | 2.1419 mL | |
| 50 mM | 0.0685 mL | 0.3427 mL | 0.6854 mL | 1.7135 mL |
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