DS-437
Based on 1 publication(s) in Google Scholar
DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3.
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- Reinheit: 99.22%
- CAS. Nr.: 1674364-87-4
- Formel: C15H23N7O4S
- Molecular Weight:397.45
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
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Publications Citing Use of MedChemExpress (MCE) DS-437
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Biologische Aktivität
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PRMT5 |
PRMT7 |
FOXP3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
>50 μM
Compound: DS-437
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Inhibition of human full length DNMT3A expressed in Sf9 cells
Inhibition of human full length DNMT3A expressed in Sf9 cells
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[PMID: 25893041] |
| Sf9 | IC50 |
>50 μM
Compound: DS-437
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Inhibition of human full length DNMT3B expressed in Sf9 cells
Inhibition of human full length DNMT3B expressed in Sf9 cells
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[PMID: 25893041] |
| Sf9 | IC50 |
>50 μM
Compound: DS-437
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Inhibition of human full length PRMT5 expressed in Sf9 cells
Inhibition of human full length PRMT5 expressed in Sf9 cells
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[PMID: 25893041] |
| Sf9 | IC50 |
>50 μM
Compound: DS-437
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Inhibition of human full length PRMT7 expressed in Sf9 cells
Inhibition of human full length PRMT7 expressed in Sf9 cells
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[PMID: 25893041] |
| Sf9 | IC50 |
37 μM
Compound: DS-437
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Inhibition of human full length PRMT5-MEP50 complex expressed in Sf9 cells using full length histone H4 substrate
Inhibition of human full length PRMT5-MEP50 complex expressed in Sf9 cells using full length histone H4 substrate
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[PMID: 25893041] |
| Sf9 | IC50 |
5.9 μM
Compound: DS-437
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Inhibition of human full length PRMT5-MEP50 complex expressed in Sf9 cells
Inhibition of human full length PRMT5-MEP50 complex expressed in Sf9 cells
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[PMID: 25893041] |
| Sf9 | IC50 |
6 μM
Compound: DS-437
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Inhibition of human full length PRMT7 expressed in Sf9 cells assessed as inhibition of H2B[23-37] methylation
Inhibition of human full length PRMT7 expressed in Sf9 cells assessed as inhibition of H2B[23-37] methylation
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[PMID: 25893041] |
DS-437 was able to inhibit methylation of an H4[1–24] peptide by the PRMT5–MEP50 complex under balanced conditions (cofactor and substrate concentrations set at their respective Km values) in a dose-dependent manner with an IC50 of 5.9 ± 1.4 μM[1].
DS-437 increased total CD8+ and CD8+ PD-1+ T cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six to Ten weeks old female Balb/c mice (bearing CT26Her2 tumor cells)[1]
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Dosage:10 mg/kg
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Administration:i.p.; 5 times a week
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Result:Had some beneficial effects on inhibiting tumor growth.
Chemical Information
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CAS. Nr. 1674364-87-4
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Appearance Solid
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Molecular Weight 397.45
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Formel C15H23N7O4S
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Color Light brown to brown
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SMILES
O[C@@H]([C@H]([C@H](N1C=NC2=C(N=CN=C21)N)O3)O)[C@H]3CSCCNC(NCC)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
The interaction between UBR7 and PRMT5 drives PDAC resistance to gemcitabine by regulating glycolysis and immune microenvironment. [Abstract]2024 Oct 18;15(10):758. PMID: 39424627
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (314.50 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (5.23 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.23 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Smil D, et al. Discovery of a Dual PRMT5-PRMT7 Inhibitor.ACS Med Chem Lett. 2015 Mar 2;6(4):408-12. [Content Brief]
[2]. Nagai Y, et al. PRMT5 Associates With the FOXP3 Homomer and When Disabled Enhances Targetedp185erbB2/neu Tumor Immunotherapy.Front Immunol. 2019 Feb 8;10:174. [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 | 2.5160 mL | 12.5802 mL | 25.1604 mL | 62.9010 mL |
| 5 mM | 0.5032 mL | 2.5160 mL | 5.0321 mL | 12.5802 mL | |
| 10 mM | 0.2516 mL | 1.2580 mL | 2.5160 mL | 6.2901 mL | |
| 15 mM | 0.1677 mL | 0.8387 mL | 1.6774 mL | 4.1934 mL | |
| 20 mM | 0.1258 mL | 0.6290 mL | 1.2580 mL | 3.1450 mL | |
| 25 mM | 0.1006 mL | 0.5032 mL | 1.0064 mL | 2.5160 mL | |
| 30 mM | 0.0839 mL | 0.4193 mL | 0.8387 mL | 2.0967 mL | |
| 40 mM | 0.0629 mL | 0.3145 mL | 0.6290 mL | 1.5725 mL | |
| 50 mM | 0.0503 mL | 0.2516 mL | 0.5032 mL | 1.2580 mL | |
| 60 mM | 0.0419 mL | 0.2097 mL | 0.4193 mL | 1.0483 mL | |
| 80 mM | 0.0315 mL | 0.1573 mL | 0.3145 mL | 0.7863 mL | |
| 100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.6290 mL |
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