DNMT/HDAC-IN-1
Based on 1 Customer Validation
DNMT/HDAC-IN-1 (Compund 15a) is a dual DNMT and HDAC inhibitor with IC50 values for HDAC1 and HDAC6 are 56.84 nM and 17.39 nM respectively. DNMT/HDAC-IN-1 can induce apoptosis and be used in tumor research.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 2095619-17-1
- Formula: C19H16ClF3N2O3
- Molecular Weight:412.79
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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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Biological Activity
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HDAC1 56.84 nM (IC50) |
HDAC6 17.39 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
2.85 μM
Compound: 15a
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Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
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[PMID: 28419930] |
| U-937 | IC50 |
1.06 μM
Compound: 15a
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Antiproliferative activity against human U937 cells after 72 hrs by MTT assay
Antiproliferative activity against human U937 cells after 72 hrs by MTT assay
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[PMID: 28419930] |
DNMT/HDAC-IN-1 significantly suppress K562 and U937 proliferation with IC50 values of 2.85 and 1.06 mM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U937 cells
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Concentration:0, 1, 2.5, 5 μM
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Incubation Time:12 h
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Result:induced histone H3K9 and histone H4K8 acetylation and increased P16 expression.
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Cell Line:U937 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:36 h
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Result:induced apoptosis in U937 cells.
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Animal Model:female BALB/c wild-type mice[2]
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Dosage:50 mg/kg
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Administration:I.v.; daily; 21 days
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Result:inhibited tumor growth.
Chemical Information
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CAS No. 2095619-17-1
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Appearance Solid
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Molecular Weight 412.79
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Formula C19H16ClF3N2O3
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Color White to off-white
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SMILES
O=C(NO)/C=C/C1=CC=C(C=C1)CCNC(C2=C(C=CC(C(F)(F)F)=C2)Cl)=O
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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)
Solvent & Solubility
DMSO : 100 mg/mL (242.25 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, 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: ≥ 2.5 mg/mL (6.06 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. * 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 (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Yuan Z, et al. Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors. Eur J Med Chem. 2017 Jul 7;134:281-292. [Content Brief]
[2]. Huang W, et al. Dual inhibitors of DNMT and HDAC induce viral mimicry to induce antitumour immunity in breast cancer. Cell Death Discov. 2024 Mar 15;10(1):143. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4225 mL | 12.1127 mL | 24.2254 mL | 60.5635 mL |
| 5 mM | 0.4845 mL | 2.4225 mL | 4.8451 mL | 12.1127 mL | |
| 10 mM | 0.2423 mL | 1.2113 mL | 2.4225 mL | 6.0563 mL | |
| 15 mM | 0.1615 mL | 0.8075 mL | 1.6150 mL | 4.0376 mL | |
| 20 mM | 0.1211 mL | 0.6056 mL | 1.2113 mL | 3.0282 mL | |
| 25 mM | 0.0969 mL | 0.4845 mL | 0.9690 mL | 2.4225 mL | |
| 30 mM | 0.0808 mL | 0.4038 mL | 0.8075 mL | 2.0188 mL | |
| 40 mM | 0.0606 mL | 0.3028 mL | 0.6056 mL | 1.5141 mL | |
| 50 mM | 0.0485 mL | 0.2423 mL | 0.4845 mL | 1.2113 mL | |
| 60 mM | 0.0404 mL | 0.2019 mL | 0.4038 mL | 1.0094 mL | |
| 80 mM | 0.0303 mL | 0.1514 mL | 0.3028 mL | 0.7570 mL | |
| 100 mM | 0.0242 mL | 0.1211 mL | 0.2423 mL | 0.6056 mL |
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