2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. ML364

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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ML364 Chemical Structure

ML364 Chemical Structure

CAS No. : 1991986-30-1

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10 mM * 1 mL in DMSO
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Customer Review

Based on 14 publication(s) in Google Scholar

ML364 Related Antibodies

Top Publications Citing Use of Products

    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.

    View All Deubiquitinase Isoform Specific Products:

    View All Isoforms
    USP1 USP2 USP7 USP8 USP30 UCHL1

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2].

    IC50 & Target

    IC50: 1.1 μM (USP2)[1]
    Kd: 5.2 μM (USP2)[1]
    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 EC50
    3.6 μM
    Compound: Fig 49, Cpd ML-364
    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
    		[PMID: 32092586]
    In Vitro

    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.

    ML364 Related Antibodies

    Cell Viability Assay[1]

    Cell Line: LnCAP, MCF7 cells
    Concentration: 5, 10, 15, 20 μM
    Incubation Time: 24, 48 hours
    Result: LnCAP and MCF7 cells showed a decrease in cell viability in a dose-dependent manner.

    Western Blot Analysis[1]

    Cell Line: HCT116, Mino cells
    Concentration: 2, 4, 8, 16, 24 hours
    Incubation Time: 10 μM
    Result: Reduced cyclin D1 protein levels in a time-, dose-, and proteasome-dependent manner in HCT116 cells and Mino cells.
    Molecular Weight

    517.54

    Formula

    C24H18F3N3O3S2
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    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
    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 (96.61 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 1.9322 mL 9.6611 mL 19.3222 mL
    5 mM 0.3864 mL 1.9322 mL 3.8644 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
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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 (4.83 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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:  0.5% CMC-Na/saline water

      Solubility: 20 mg/mL (38.64 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

    Purity: 99.96%

    SDS (393 KB)

    COA (253 KB) HNMR (138 KB) RP-HPLC (241 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    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 1.9322 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
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    ML364 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:

    ML3641991986-30-1ML 364ML-364DeubiquitinaseDUBsInhibitorinhibitorinhibit

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