EWP 815
Based on 1 Customer Validation
EWP 815 is a disulfiram analogue, is a potent inhibitor of Ins(1,4)P2 phosphatase and Ins(1,4,5)P3 5-phosphatase. EWP 815 also inhibits enzyme dopamine β-hydroxylase activity.
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- Pureza: 99.15%
- No. CAS: 20231-01-0
- Fòrmula: C12H22N4S4
- Peso molecular:350.59
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Ins(1,4)P2 phosphatase; Ins(1,4,5)P3 5-phosphatase[1]; dopamine β-hydroxylase[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF-10A | IC50 |
>10 μM
Compound: 3b
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Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay
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[PMID: 20222671] |
| MCF7 | IC50 |
0.35 μM
Compound: 3b
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Antiproliferative activity against human MCF7 cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay
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[PMID: 20222671] |
| MDA-MB-231 | IC50 |
0.29 μM
Compound: 3b
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Antiproliferative activity against human MDA-MB-231 cells expressing BCA2 and ERalpha after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells expressing BCA2 and ERalpha after 72 hrs by MTT assay
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[PMID: 20222671] |
| MDA-MB-231 | IC50 |
3 μM
Compound: 3b
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Antiproliferative activity against BCA2 and ER deficient human MDA-MB-231 cells after 72 hrs by MTT assay
Antiproliferative activity against BCA2 and ER deficient human MDA-MB-231 cells after 72 hrs by MTT assay
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[PMID: 20222671] |
| T47D | IC50 |
0.33 μM
Compound: 3b
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Antiproliferative activity against human T47D cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay
Antiproliferative activity against human T47D cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay
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[PMID: 20222671] |
EWP 815 inhibits thyrotropin-releasing hormone (TRH; 0.03 mM)-stimulated inositol phospholipid breakdown without affecting basal breakdown rates in prelabelled GH3 cells with IC50s of 83 mM (soluble enzymes) and 71 mM (particulate enzymes), respectively[1].
EWP 815 (30 μM; 1 h) exerts higher inhibition on Ins(1,4)P2 phosphatase rather than Ins(1,4,5)P3 5-phosphatase with the mean [3H]Ins(1,4)P2/mean [3H]InsP recovery ratio of 2.6[1].
EWP 815 (6, 8 μM; 10 min) inhibits dephosphorylation of [3H]Ins(1,4,5)P3 5-phosphatase in particulate and soluble fractions with IC50s of 6 μM and 8 μM, respectively[1].
EWP 815 (3-300 μM; 30 min) suppresses thyrotropin-releasing hormone (TRH)-stimulated (100 nM) inositol phospholipid production by 30% (100 μM) and 1.8% (300 μM), respectively, without affecting Ins(1,4,5)P3 binding[1].
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:Female mice (20 g)[2]
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Dosage:50 mg/kg
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Administration:Intraperitoneal injection; 30 min before killed
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Result:Intraperitoneal injection; 30 min before killedInhibited β-hydroxylase of 3H-α-methyldopamine.
Reduced the amount of 3H-α-Me-NA by 12%.
Chemical Information
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No. CAS 20231-01-0
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Appearance Solid
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Peso molecular 350.59
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Fòrmula C12H22N4S4
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Color White to off-white
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SMILES
S=C(N1CCN(C)CC1)SSC(N2CCN(C)CC2)=S
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 50 mg/mL (142.62 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.57 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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. * 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.
Pureza y Documentación
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Ficha de datos (283 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Fowler CJ, et al. Inhibition of inositol 1,4,5-trisphosphate 5-phosphatase by micromolar concentrations of disulfiram and its analogues. Biochem J. 1993 Feb 1;289 ( Pt 3)(Pt 3):853-9. [Content Brief]
[2]. Carlsson A, et al. On the beta-hydroxylation of (+-)-alpha-methyldopamine in vivo. Eur J Pharmacol. 1968 Dec;5(1):85-92. [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 | 2.8523 mL | 14.2617 mL | 28.5233 mL | 71.3084 mL |
| 5 mM | 0.5705 mL | 2.8523 mL | 5.7047 mL | 14.2617 mL | |
| 10 mM | 0.2852 mL | 1.4262 mL | 2.8523 mL | 7.1308 mL | |
| 15 mM | 0.1902 mL | 0.9508 mL | 1.9016 mL | 4.7539 mL | |
| 20 mM | 0.1426 mL | 0.7131 mL | 1.4262 mL | 3.5654 mL | |
| 25 mM | 0.1141 mL | 0.5705 mL | 1.1409 mL | 2.8523 mL | |
| 30 mM | 0.0951 mL | 0.4754 mL | 0.9508 mL | 2.3769 mL | |
| 40 mM | 0.0713 mL | 0.3565 mL | 0.7131 mL | 1.7827 mL | |
| 50 mM | 0.0570 mL | 0.2852 mL | 0.5705 mL | 1.4262 mL | |
| 60 mM | 0.0475 mL | 0.2377 mL | 0.4754 mL | 1.1885 mL | |
| 80 mM | 0.0357 mL | 0.1783 mL | 0.3565 mL | 0.8914 mL | |
| 100 mM | 0.0285 mL | 0.1426 mL | 0.2852 mL | 0.7131 mL |
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