DNMT1/HDAC-IN-1
DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC50=0.05 μM), HDAC1 is a major HDAC isoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities.
For research use only. We do not sell to patients.
- CAS No.: 3104460-09-2
- Formula: C33H35N7O3S
- Molecular Weight:609.74
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
All DNA Methyltransferase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
HDAC1 0.05 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
0.36 μM
Compound: (R)-23a
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Inhibition of cell viability in human HL-60 cells incubated for 4 days by CCK8 assay
Inhibition of cell viability in human HL-60 cells incubated for 4 days by CCK8 assay
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[PMID: 39264152] |
| Kasumi 1 | IC50 |
0.41 μM
Compound: (R)-23a
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Inhibition of cell viability in human Kasumi 1 cells incubated for 4 days by CCK8 assay
Inhibition of cell viability in human Kasumi 1 cells incubated for 4 days by CCK8 assay
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[PMID: 39264152] |
| MV4-11 | IC50 |
0.32 μM
Compound: (R)-23a
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Inhibition of cell viability in human MV4-11 cells incubated for 4 days by CCK8 assay
Inhibition of cell viability in human MV4-11 cells incubated for 4 days by CCK8 assay
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[PMID: 39264152] |
Chemical Information
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CAS No. 3104460-09-2
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Molecular Weight 609.74
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Formula C33H35N7O3S
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SMILES
CCC1=C(C(S[C@H](C2=CC=CC=C2)C(N)=O)=NC(N3CCC(CC3)CNCC4=CC=C(C=C4)/C=C/C(NO)=O)=C1C#N)C#N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 200 mg/mL (328.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 5 mg/mL (8.20 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
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
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6400 mL | 8.2002 mL | 16.4004 mL | 41.0011 mL |
| 5 mM | 0.3280 mL | 1.6400 mL | 3.2801 mL | 8.2002 mL | |
| 10 mM | 0.1640 mL | 0.8200 mL | 1.6400 mL | 4.1001 mL | |
| 15 mM | 0.1093 mL | 0.5467 mL | 1.0934 mL | 2.7334 mL | |
| 20 mM | 0.0820 mL | 0.4100 mL | 0.8200 mL | 2.0501 mL | |
| 25 mM | 0.0656 mL | 0.3280 mL | 0.6560 mL | 1.6400 mL | |
| 30 mM | 0.0547 mL | 0.2733 mL | 0.5467 mL | 1.3667 mL | |
| 40 mM | 0.0410 mL | 0.2050 mL | 0.4100 mL | 1.0250 mL | |
| 50 mM | 0.0328 mL | 0.1640 mL | 0.3280 mL | 0.8200 mL | |
| 60 mM | 0.0273 mL | 0.1367 mL | 0.2733 mL | 0.6834 mL | |
| 80 mM | 0.0205 mL | 0.1025 mL | 0.2050 mL | 0.5125 mL | |
| 100 mM | 0.0164 mL | 0.0820 mL | 0.1640 mL | 0.4100 mL |
DNMT1/HDAC-IN-1 Related Classifications
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