MALT1 inhibitor MI-2 [1047953-91-2]

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MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals.

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MALT1 inhibitor MI-2 Chemical Structure

MALT1 inhibitor MI-2 Chemical Structure

CAS No. : 1047953-91-2

This product is a controlled substance and not for sale in your territory.

Based on 6 publication(s) in Google Scholar

    MALT1 inhibitor MI-2 purchased from MedChemExpress. Usage Cited in: Parasit Vectors. 2018 May 18;11(1):305.  [Abstract]

    The A20 protein levels in Jurkat T-cells and Molt-4 T-cells treated with MALT1 inhibitor MI-2 and combined use of MI-2 and ME-49.
    Description

    MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals[1].

    IC50 & Target

    IC50: 5.84 μM (MALT1)[1]

    Cellular Effect
    Cell Line Type Value Description References
    OCI-Ly3 IC50
    2.6 μM
    Compound: MI-2
    Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTT assay
    Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTT assay
    [PMID: 26496175]
    Toledo IC50
    0.8 μM
    Compound: 11; MI-2
    Antiproliferative activity against human Toledo cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human Toledo cells after 48 hrs by CCK8 assay
    [PMID: 29751989]
    In Vitro

    MALT1 inhibitor MI-2 (1-1000 nM; 48 hours) selectively suppresses MALT1-dependent DLBCL cell lines, and the GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells is 0.2, 0.5, 0.4, and 0.4 μM, respectively[1].
    ? MALT1 inhibitor MI-2 (62-1000 nM; 24 hours) causes a dose-dependent decrease in MALT1-mediated cleavage[1].

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

    Cell Proliferation Assay[1]

    Cell Line: HBL-1, TMD8, OCI-Ly3, OCI-Ly10 cells
    Concentration: 1, 10, 100, 1000 nM
    Incubation Time: 48 hours
    Result: The GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells was 0.2, 0.5, 0.4, and 0.4 µM, respectively.

    Western Blot Analysis[1]

    Cell Line: HBL-1 cells
    Concentration: 62, 125, 250, 500, 1000 nM
    Incubation Time: 24 hours
    Result: Inhibits MALT1 cleavage of CYLD in HBL-1 cells.
    In Vivo

    MALT1 inhibitor MI-2 (25 mg/kg; i.p.; daily for 14 days) profoundly suppresses the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts[1].

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

    Animal Model: Eight-week-old male SCID NOD (bearing HBL-1 and TMD8 cells)[1]
    Dosage: 25 mg/kg
    Administration: Intraperitoneal injection; daily for 14 days
    Result: Profoundly suppressed the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts versus vehicle.
    Masse moléculaire

    455.72

    Formule

    C19H17Cl3N4O3

    CAS No.

    1047953-91-2

    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CC=C(N2N=C(OCCOC)N=C2C3=CC=C(Cl)C(Cl)=C3)C=C1)CCl

    Livraison

    Room temperature in continental US; may vary elsewhere.

    Stockage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvant et solubilité
    In Vitro: 

    DMSO : ≥ 46 mg/mL (100.94 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1943 mL 10.9716 mL 21.9433 mL
    5 mM 0.4389 mL 2.1943 mL 4.3887 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.

    • Calculateur de molarité

    • Calculateur de dilution

    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 (5.49 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 (5.49 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.

    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.
    Pureté et documentation

    Purity: 99.95%

    Références
    • [1]. Fontan L, et al. MALT1 small molecule inhibitors specifically suppress ABC-DLBCL in vitro and in vivo. Cancer Cell. 2012 Dec 11;22(6):812-24.  [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 2.1943 mL 10.9716 mL 21.9433 mL 54.8582 mL
    5 mM 0.4389 mL 2.1943 mL 4.3887 mL 10.9716 mL
    10 mM 0.2194 mL 1.0972 mL 2.1943 mL 5.4858 mL
    15 mM 0.1463 mL 0.7314 mL 1.4629 mL 3.6572 mL
    20 mM 0.1097 mL 0.5486 mL 1.0972 mL 2.7429 mL
    25 mM 0.0878 mL 0.4389 mL 0.8777 mL 2.1943 mL
    30 mM 0.0731 mL 0.3657 mL 0.7314 mL 1.8286 mL
    40 mM 0.0549 mL 0.2743 mL 0.5486 mL 1.3715 mL
    50 mM 0.0439 mL 0.2194 mL 0.4389 mL 1.0972 mL
    60 mM 0.0366 mL 0.1829 mL 0.3657 mL 0.9143 mL
    80 mM 0.0274 mL 0.1371 mL 0.2743 mL 0.6857 mL
    100 mM 0.0219 mL 0.1097 mL 0.2194 mL 0.5486 mL
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    MALT1 inhibitor MI-2 Related Classifications

    Help & FAQs

    Keywords:

    MALT1 inhibitor MI-21047953-91-2MALT1mucosa associated lymphoid tissue lymphoma translocation gene 1Inhibitorinhibitorinhibit

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