ML364
Based on 22 publication(s) in Google Scholar
ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP.
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- Pureté: 99.96%
- CAS No.: 1991986-30-1
- Formule: C24H18F3N3O3S2
- Masse moléculaire:517.54
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) ML364
More- Nat Commun. 2025 May 16;16(1):4564. [Abstract]
- Nat Commun. 2022 Mar 31;13(1):1700. [Abstract]
- Cell Death Differ. 2020 Sep;27(9):2710-2725. [Abstract]
- Redox Biol. 2026 May:92:104086. [Abstract]
- J Immunother Cancer. 2026 Jan 14;14(1):e013498. [Abstract]
- Cell Death Dis. 2025 Aug 28;16(1):654. [Abstract]
- EMBO J. 2022 Aug 16;41(16):e108791. [Abstract]
- J Med Chem. 2022 Oct 27;65(20):13645-13659. [Abstract]
- Inflamm Res. 2026 Mar 17;75(1):60. [Abstract]
- FASEB J. 2021 Aug;35(8):e21800. [Abstract]
- J Cell Mol Med. 2021 Jan;25(2):1001-1011. [Abstract]
- Mol Cell Biochem. 2024 Apr;479(4):843-857. [Abstract]
- Anim Cells Syst. 2024 May 11;28(1):237-250. [Abstract]
- Arch Biochem Biophys. 2024 Oct 30:762:110193. [Abstract]
- Am J Cancer Res. 2021 Oct 15;11(10):4746-4767. [Abstract]
- J Cancer Res Clin Oncol. 2023 Sep;149(11):9263-9276. [Abstract]
- Physiol Rep. 2019 Jul;7(14):e14193. [Abstract]
- Biomed Res. 2025;46(5):203-214. [Abstract]
- Exp Anim. 2025 Jul 19. [Abstract]
- bioRxiv. 2025 May 14.
- Preprints. 2024 Jul 31.
- University of Adelaide. 2023 Jan.
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IF
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | EC50 |
3.6 μM
Compound: Fig 49, Cpd ML-364
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Anticancer activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Anticancer activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
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[PMID: 32092586] |
| HCT-116 | IC50 |
1.1 μM
Compound: 48; ML364
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 38262120] |
| MCF-10A | IC50 |
14.5 μM
Compound: ML364
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Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38452725] |
| MCF7 | IC50 |
9.3 μM
Compound: ML364
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38452725] |
ML364 (5-20 μM; 24-48 hours) inhibits LnCAP and MCF7 cells viability in a dose-dependent manner[1].
ML364 (10 μM; 2-24 hours) reduces cyclin D1 protein levels in a time-, dose-, and proteasome-dependent manner in HCT116 cells and Mino cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LnCAP, MCF7 cells
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Concentration:5, 10, 15, 20 μM
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Incubation Time:24, 48 hours
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Result:LnCAP and MCF7 cells showed a decrease in cell viability in a dose-dependent manner.
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Cell Line:HCT116, Mino cells
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Concentration:2, 4, 8, 16, 24 hours
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Incubation Time:10 μM
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Result:Reduced cyclin D1 protein levels in a time-, dose-, and proteasome-dependent manner in HCT116 cells and Mino cells.
Chemical Information
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CAS No. 1991986-30-1
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Appearance Solid
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Masse moléculaire 517.54
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Formule C24H18F3N3O3S2
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Color White to light yellow
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SMILES
O=C(NC1=NC(C2=CC=CC=C2)=CS1)C3=CC=C(C(F)(F)F)C=C3NS(=O)(C4=CC=C(C)C=C4)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (22)
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Journal Impact Factor
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Most Recent
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Nat Commun
2025 May 16;16(1):4564. PMID: 40379682 -
Nat Commun
USP8 inhibition reshapes an inflamed tumor microenvironment that potentiates the immunotherapy. [Abstract]2022 Mar 31;13(1):1700. PMID: 35361799 -
Cell Death Differ
The deubiquitylase USP2 maintains ErbB2 abundance via counteracting endocytic degradation and represents a therapeutic target in ErbB2-positive breast cancer. [Abstract]2020 Sep;27(9):2710-2725. PMID: 32327714 -
Redox Biol
USP20 governs tyrosine kinase inhibitors resistance through ferroptosis evasion by targeting GPX4 in cancers. [Abstract]2026 May:92:104086. PMID: 41844497 -
J Immunother Cancer
CD47 destabilization via manipulating the SPOP-USP2 axis augments macrophage phagocytosis and cancer immunotherapy. [Abstract]2026 Jan 14;14(1):e013498. PMID: 41534899 -
Cell Death Dis
DCAF7 recruits USP2 to facilitate hepatocellular carcinoma progression by suppressing clockophagy-induced ferroptosis. [Abstract]2025 Aug 28;16(1):654. PMID: 40877242 -
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 -
J Med Chem
Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. [Abstract]2022 Oct 27;65(20):13645-13659. PMID: 36221183 -
Inflamm Res
2026 Mar 17;75(1):60. PMID: 41843135 -
FASEB J
2021 Aug;35(8):e21800. PMID: 34324733 -
J Cell Mol Med
Ubiquitin-specific protease 2 regulates Ang Ⅱ-induced cardiac fibroblasts activation by up-regulating cyclin D1 and stabilizing β-catenin in vitro. [Abstract]2021 Jan;25(2):1001-1011. PMID: 33314748 -
Mol Cell Biochem
A novel 2-iminobenzimidazole compound, XYA1353, displays in vitro and in vivo anti-myeloma activity via targeting NF-κB signaling. [Abstract]2024 Apr;479(4):843-857. PMID: 37204666 -
Anim Cells Syst
Blocking SLC7A11 attenuates the proliferation of esophageal squamous cell carcinoma cells. [Abstract]2024 May 11;28(1):237-250. PMID: 38741950 -
Arch Biochem Biophys
Pharmacological USP2 targeting suppresses ovarian cancer growth by potentiating apoptosis and ferroptosis. [Abstract]2024 Oct 30:762:110193. PMID: 39486565 -
Am J Cancer Res
Dysregulation and activities of ubiquitin specific peptidase 2b in the pathogenesis of hepatocellular carcinoma. [Abstract]2021 Oct 15;11(10):4746-4767. PMID: 34765291 -
J Cancer Res Clin Oncol
USP2 promotes cell proliferation and metastasis in choroidal melanoma via stabilizing Snail. [Abstract]2023 Sep;149(11):9263-9276. PMID: 37199836 -
Physiol Rep
Inhibition of ubiquitin-specific protease 2 causes accumulation of reactive oxygen species, mitochondria dysfunction, and intracellular ATP decrement in C2C12 myoblasts. [Abstract]2019 Jul;7(14):e14193. PMID: 31353872
ML364 purchased from MedChemExpress. Usage Cited in: Physiol Rep. 2019 Jul;7(14):e14193. [Abstract]
Effects of ML364 on cytotoxicity, proliferation, intracellular level of ATP, mitochondrial membrane potential, mitochondria morphology, and accumulation of ROS in C2C12 cells.
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Biomed Res
Muscular USP2 is dispensable for MASLD-associated disorders in the liver and skeletal muscle in mice. [Abstract]2025;46(5):203-214. PMID: 41016774 -
Exp Anim
Suppression of USP2 in mouse skeletal muscle: a model of oxidative stress in muscle tissue. [Abstract]2025 Jul 19. PMID: 40691076 -
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Solvant et solubilité
DMSO : 50 mg/mL (96.61 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.
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: 0.5% CMC-Na/saline water
Solubility: 20 mg/mL (38.64 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.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Davis MI, et al. Small Molecule Inhibition of the Ubiquitin-specific Protease USP2 Accelerates cyclin D1 Degradation and Leads to Cell Cycle Arrest in Colorectal Cancer and Mantle Cell Lymphoma Models. J Biol Chem. 2016 Nov 18;291(47):24628-24640. [Content Brief]
[2]. Hashimoto M, et al. Inhibition of ubiquitin-specific protease 2 causes accumulation of reactive oxygen species, mitochondria dysfunction, and intracellular ATP decrement in C2C12 myoblasts. Physiol Rep. 2019 Jul;7(14):e14193. [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 | 1.9322 mL | 9.6611 mL | 19.3222 mL | 48.3054 mL |
| 5 mM | 0.3864 mL | 1.9322 mL | 3.8644 mL | 9.6611 mL | |
| 10 mM | 0.1932 mL | 0.9661 mL | 1.9322 mL | 4.8305 mL | |
| 15 mM | 0.1288 mL | 0.6441 mL | 1.2881 mL | 3.2204 mL | |
| 20 mM | 0.0966 mL | 0.4831 mL | 0.9661 mL | 2.4153 mL | |
| 25 mM | 0.0773 mL | 0.3864 mL | 0.7729 mL | 1.9322 mL | |
| 30 mM | 0.0644 mL | 0.3220 mL | 0.6441 mL | 1.6102 mL | |
| 40 mM | 0.0483 mL | 0.2415 mL | 0.4831 mL | 1.2076 mL | |
| 50 mM | 0.0386 mL | 0.1932 mL | 0.3864 mL | 0.9661 mL | |
| 60 mM | 0.0322 mL | 0.1610 mL | 0.3220 mL | 0.8051 mL | |
| 80 mM | 0.0242 mL | 0.1208 mL | 0.2415 mL | 0.6038 mL |