2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. EOAI3402143

EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5.

For research use only. We do not sell to patients.

EOAI3402143 Chemical Structure

EOAI3402143 Chemical Structure

CAS No. : 1699750-95-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 199 In-stock
Solution
10 mM * 1 mL in DMSO USD 199 In-stock
Solid
5 mg USD 180 In-stock
10 mg USD 290 In-stock
25 mg USD 570 In-stock
50 mg USD 912 In-stock
100 mg USD 1460 In-stock
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500 mg   Get quote  

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Customer Review

Based on 8 publication(s) in Google Scholar

EOAI3402143 Related Antibodies

Top Publications Citing Use of Products

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USP1 USP2 USP7 USP8 USP30 UCHL1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5.

IC50 & Target

Usp5[1]
Usp9x[1][2][3]
Usp24[2]
In Vitro

EOAI3402143 retains potent Usp9x and Usp5 inhibitory activity[1]. EOAI3402143 dose-dependently inhibits Usp9x and Usp24 activity, increases tumor cell apoptosis[2]. Treatment of UM-2, UM-6, UM-16, and UM-76 with Usp9x inhibitor EOAI3402143 (G9) dose-dependently suppresses cell survival, while 600 nM of EOAI3402143 completely suppresses UM-2 3D colony growth when compared to untreated vehicle controls[3].

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

EOAI3402143 Related Antibodies
In Vivo

To examine this potential, the effect of EOAI3402143 (G9) treatment is investigated on human MIAPACA2 tumor xenografts. Human MIAPACA2 cells are injected subcutaneously into NSG mice. Primary tumor development is monitored by caliper measurements, and once measurable, mice are separated into two groups and are treated with either vehicle control (PEG300/DMSO) or G9 at 15 mg/kg. Tumor growth, animal weight, behavior, and mobility are monitored during treatment. In parallel, murine 8041 tumors are also established and subjected to similar G9 treatment and tumor monitoring regimen as the human MIAPACA2 xenografts. Consistent with the in vitro findings, Usp9x inhibition results in the suppression of tumor growth in human tumor xenografts, but any significant effect on the growth of 8041 tumors xenografts is not observed, although the Usp9x activity is inhibited effectively by EOAI3402143 treatment in both human MIAPACA2 and mouse 8041 xenograft tumors[3].

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

503.42

Formula

C25H28Cl2N4O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=C(/C=C(C(NC(CCC)C2=CC=C(OCCN3CCOCC3)C=C2)=O)\C#N)N=C(Cl)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (99.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9864 mL 9.9321 mL 19.8641 mL
5 mM 0.3973 mL 1.9864 mL 3.9728 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.97 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.97 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 10 mg/mL (19.86 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
Cell Assay
[3]

UM-2, UM-6, UM-16, and UM-76 cells are seeded in a 96-well plate at 5000 per well in the presence of the indicated concentration of EOAI3402143 (1, 2, 3, 4, and 5 μM) for 3 days in a CO2 incubator at 37°C. Twenty microliters of 5 g/L MTT solution are added to each well for 2 hours at 37°C. The cells are then lysed in 10% SDS buffer, and absorbance at 570 nm relative to a reference wavelength of 630 nm is determined with a microplate reader. To examine proliferation using the MTT assay, cells are plated in triplicates, and the samples are processed for MTT assay at day 0, 1, 2, 3, and 4[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Mice[3]
NSG [NOD/SCID/IL2r-g (null)] mice are injected mid-dorsally with 2×106 8041 or 5×106 MIAPACA2 cells in 0.1 mL of Matrigel/DMEM suspension. Tumors are allowed to establish to about 100 mm3, after which mice are tumor size matched and allocated to five per treatment group (vehicle or EOAI3402143) for 8041 tumor-bearing mice and four per treatment group for MIAPACA2 tumor-bearing mice. EOAI3402143 is administered in DMSO:PEG300 (1:1) by i.p injection every other day at 15 mg/kg. Tumor size is monitored by caliper measurements twice a week, and tumor volume is calculated[3].

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

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 1.9864 mL 9.9321 mL 19.8641 mL 49.6603 mL
5 mM 0.3973 mL 1.9864 mL 3.9728 mL 9.9321 mL
10 mM 0.1986 mL 0.9932 mL 1.9864 mL 4.9660 mL
15 mM 0.1324 mL 0.6621 mL 1.3243 mL 3.3107 mL
20 mM 0.0993 mL 0.4966 mL 0.9932 mL 2.4830 mL
25 mM 0.0795 mL 0.3973 mL 0.7946 mL 1.9864 mL
30 mM 0.0662 mL 0.3311 mL 0.6621 mL 1.6553 mL
40 mM 0.0497 mL 0.2483 mL 0.4966 mL 1.2415 mL
50 mM 0.0397 mL 0.1986 mL 0.3973 mL 0.9932 mL
60 mM 0.0331 mL 0.1655 mL 0.3311 mL 0.8277 mL
80 mM 0.0248 mL 0.1242 mL 0.2483 mL 0.6208 mL
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EOAI3402143 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EOAI34021431699750-95-2EOAI 3402143EOAI-3402143DeubiquitinaseDUBsInhibitorinhibitorinhibit

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