Art. -Nr.: HY-148001

EWP 815

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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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Reinheit: 99.15%
CAS. Nr.: 20231-01-0
Formel: C₁₂H₂₂N₄S₄
Molecular Weight:350.59

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

EWP 815 Chemical Structure

CAS. Nr.: 20231-01-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]^[2].

IC₅₀ & Target

Ins(1,4)P2 phosphatase; Ins(1,4,5)P3 5-phosphatase^[1]; dopamine β-hydroxylase^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
MCF-10A	IC₅₀	>10 μM Compound: 3b	Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay	[PMID: 20222671]
MCF7	IC₅₀	0.35 μM Compound: 3b	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	[PMID: 20222671]
MDA-MB-231	IC₅₀	0.29 μM Compound: 3b	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	[PMID: 20222671]
MDA-MB-231	IC₅₀	3 μM Compound: 3b	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	[PMID: 20222671]
T47D	IC₅₀	0.33 μM Compound: 3b	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	[PMID: 20222671]

In Vitro

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.

In Vivo

EWP 815 (50 mg/kg; i.p.; 30 min before killed) inhibits the enzyme dopamine β-hydroxylase activity in mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female mice (20 g)^[2]
Dosage:

50 mg/kg
Administration:

Intraperitoneal injection; 30 min before killed
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

CAS. Nr. 20231-01-0
Appearance Solid
Molecular Weight 350.59
Formel C₁₂H₂₂N₄S₄
Color White to off-white
SMILES

S=C(N1CCN(C)CC1)SSC(N2CCN(C)CC2)=S
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8523 mL

14.2617 mL

28.5233 mL

5 mM

0.5705 mL

2.8523 mL

5.7047 mL

10 mM

0.2852 mL

1.4262 mL

2.8523 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.25 mg/mL (3.57 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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EWP 815

Metabolism/Protease Compound Library

Phosphatase Inhibitor Library

Cuproptosis Compound Library

Metabolic Enzyme Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EWP 815

Metabolism/Protease Compound Library

Phosphatase Inhibitor Library

Cuproptosis Compound Library

Metabolic Enzyme Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EWP 815 Related Classifications

HY-148001 Related Classifications