EOAI3402143
Based on 13 publication(s) in Google Scholar
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.
- Purity: 98.11%
- CAS No.: 1699750-95-2
- Formula: C25H28Cl2N4O3
- Molecular Weight:503.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
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Covalent Screening Library
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Posttranslational Modification Library
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Publications Citing Use of MedChemExpress (MCE) EOAI3402143
More- Cancer Discov. 2026 Apr 2. [Abstract]
- Mol Cell. 2020 Nov 19;80(4):633-647.e7. [Abstract]
- Nat Commun. 2025 May 16;16(1):4564. [Abstract]
- Nat Commun. 2023 May 19;14(1):2859. [Abstract]
- Acta Pharm Sin B. 2022 Apr;12(4):1856-1870. [Abstract]
- Redox Biol. 2026 May:92:104086. [Abstract]
- Cell Death Dis. 2021 Jan 7;12(1):42. [Abstract]
- EMBO J. 2022 Aug 16;41(16):e108791. [Abstract]
- Br J Pharmacol. 2024 Oct 22. [Abstract]
- Biochem Pharmacol. 2026 Feb:244:117591. [Abstract]
- Arch Pharm (Weinheim). 2023 Jul;356(7):e2200661. [Abstract]
- Patent. US20230123585A1.
- Patent. US20230123585A1.
Biological Activity
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1699750-95-2
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Appearance Solid
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Molecular Weight 503.42
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Formula C25H28Cl2N4O3
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Color Light yellow to yellow
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SMILES
ClC1=C(/C=C(C(NC(CCC)C2=CC=C(OCCN3CCOCC3)C=C2)=O)\C#N)N=C(Cl)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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Cancer Discov
HER2 heterogeneous breast cancer models reveal novel therapeutic targets and subclonal dynamics during evolution to resistance to HER2-targeted therapies. [Abstract]2026 Apr 2. PMID: 41925564 -
Mol Cell
2020 Nov 19;80(4):633-647.e7. PMID: 33217317 -
Nat Commun
2025 May 16;16(1):4564. PMID: 40379682 -
Nat Commun
ERK and USP5 govern PD-1 homeostasis via deubiquitination to modulate tumor immunotherapy. [Abstract]2023 May 19;14(1):2859. PMID: 37208329 -
Acta Pharm Sin B
Blockade of deubiquitinase YOD1 degrades oncogenic PML/RAR α and eradicates acute promyelocytic leukemia cells. [Abstract]2022 Apr;12(4):1856-1870. PMID: 35847510 -
Redox Biol
USP20 governs tyrosine kinase inhibitors resistance through ferroptosis evasion by targeting GPX4 in cancers. [Abstract]2026 May:92:104086. PMID: 41844497 -
Cell Death Dis
TRIB2 modulates proteasome function to reduce ubiquitin stability and protect liver cancer cells against oxidative stress. [Abstract]2021 Jan 7;12(1):42. PMID: 33414446 -
EMBO J
USP8 promotes cancer progression and extracellular vesicle-mediated CD8+ T cell exhaustion by deubiquitinating the TGF-β receptor TβRII. [Abstract]2022 Aug 16;41(16):e108791. PMID: 35811497 -
Br J Pharmacol
Chicoric acid exerts therapeutic effects in DSS-induced ulcerative colitis by targeting the USP9X/IGF2BP2 axis. [Abstract]2024 Oct 22. PMID: 39435543 -
Biochem Pharmacol
Deubiquitinase USP5 promotes acute myeloid leukemia through C2CD5 stabilization and PI3K/AKT/mTOR/HIF-1α-driven glycolysis. [Abstract]2026 Feb:244:117591. PMID: 41344512 -
Arch Pharm (Weinheim)
2023 Jul;356(7):e2200661. PMID: 37196427 -
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Solvent & Solubility
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)
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.
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 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.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (19.86 mM); Suspended solution; Need ultrasonic
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Potu H, et al. Usp5 links suppression of p53 and FAS levels in melanoma to the BRAF pathway. Oncotarget. 2014 Jul 30;5(14):5559-69. [Content Brief]
[2]. Peterson LF, et al. Targeting deubiquitinase activity with a novel small-molecule inhibitor as therapy for B-cell malignancies. Blood. 2015 Jun 4;125(23):3588-97. [Content Brief]
[3]. Pal A, et al. Usp9x Promotes Survival in Human Pancreatic Cancer and Its Inhibition Suppresses Pancreatic Ductal Adenocarcinoma In Vivo Tumor Growth. Neoplasia. 2018 Feb;20(2):152-164. [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 | 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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