2. Epigenetics
  3. Epigenetic Reader Domain
  4. Molibresib besylate

Molibresib besylate  (Synonyms: GSK 525762C; I-BET 762 besylate)

Cat. No.: HY-13032B Purity: 97.04%
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Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.

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

Molibresib besylate Chemical Structure

Molibresib besylate Chemical Structure

CAS No. : 1895049-20-3

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 136 In-stock
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Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of Molibresib besylate:

Molibresib besylate Related Antibodies

Top Publications Citing Use of Products

    Molibresib besylate purchased from MedChemExpress. Usage Cited in: Nat Med. 2017 Sep;23(9):1055-1062.  [Abstract]

    Western blot of WCL of C4-2 cells treated with vehicle (DMSO) or different doses of JQ1 or i-BET for 24 h. Actin is used as a loading control.

    Molibresib besylate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Jun 21;7(25):38319-38332.  [Abstract]

    iBET762 partially disrupts the interaction between full-length ERG and BRD4 (A), and between T1-E4 ERG and BRD4 (B).

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.

    IC50 & Target

    IC50: 32.5-42.5 nM (BET)[1]
    Clinical Trial
    Molecular Weight

    582.07

    Formula

    C28H28ClN5O5S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC1=CC=C(C2=N[C@@H](CC(NCC)=O)C3=NN=C(C)N3C4=CC=C(OC)C=C24)C=C1.O=S(C5=CC=CC=C5)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (42.95 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 1.7180 mL 8.5900 mL 17.1801 mL
    5 mM 0.3436 mL 1.7180 mL 3.4360 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 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: ≥ 2.67 mg/mL (4.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 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: ≥ 2.67 mg/mL (4.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 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.
    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7180 mL 8.5900 mL 17.1801 mL 42.9502 mL
    5 mM 0.3436 mL 1.7180 mL 3.4360 mL 8.5900 mL
    10 mM 0.1718 mL 0.8590 mL 1.7180 mL 4.2950 mL
    15 mM 0.1145 mL 0.5727 mL 1.1453 mL 2.8633 mL
    20 mM 0.0859 mL 0.4295 mL 0.8590 mL 2.1475 mL
    25 mM 0.0687 mL 0.3436 mL 0.6872 mL 1.7180 mL
    30 mM 0.0573 mL 0.2863 mL 0.5727 mL 1.4317 mL
    40 mM 0.0430 mL 0.2148 mL 0.4295 mL 1.0738 mL
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    Molibresib besylate 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:

    Molibresib besylate1895049-20-3GSK 525762CI-BET 762 besylateEpigenetic Reader DomainInhibitorinhibitorinhibit

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