2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. BI8622

BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM.

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

BI8622 Chemical Structure

BI8622 Chemical Structure

CAS No. : 1875036-74-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 550 In-stock
50 mg USD 1360 In-stock
100 mg USD 1900 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

BI8622 Related Antibodies

Top Publications Citing Use of Products

    BI8622 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2020 Dec 1;130(12):6301-6316.  [Abstract]

    Immunoblot analysis of pro–caspase-1 and its subunit p20. Caspase-1 activation in NLRP3, AIM2, and NLRC4 inflammasomes is substantially reduced in BMDMs treated with BI8622 (10 μM) compared with untreated BMDMs.

    BI8622 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2020 Dec;27(12):3273-3288.  [Abstract]

    Protein expression of Myst2 in Huwe1 inhibits mESCs is analyzed by Western blot using Huwe1 inhibitor (BI8622). Indicated amounts of BI8622 is treated for 24 h to inhibit Huwe1.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM[1].

    IC50 & Target

    IC50: 3.1 μM (HUWE1)[1]
    In Vitro

    BI8622 induces HUWE1 ectopically expresses to abolish ubiquitination of MCL1 with an IC50 value of 6.8 μM in HeLa cells[1].
    BI8622 suppresses colony formation of Ls174T cells with estimated IC50 value of 8.4 μM[1].
    BI8622 (10 μM; 1-4 days) treatment retards passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1[1].
    BI8622 (0-50 μM; 16 hours) retards the degradation of MCL1 in response to UV irradiation by inhibiting HUWE1 in HeLa cells[1].
    BI8622 inhibits MYC-dependent transactivation in colorectal cancer cells[1].

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

    BI8622 Related Antibodies

    Cell Cycle Analysis[1]

    Cell Line: Ls174T cells
    Concentration: 0 μM, 5 μM,10 μM, 15 μM, 20 μM
    Incubation Time: 0-4 days
    Result: Retarded passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1.

    Western Blot Analysis[1]

    Cell Line: HeLa cells
    Concentration: 0 μM, 10 μM, 20 μM
    Incubation Time: 16 hours
    Result: Retarded the degradation of MCL1 in response to UV irradiation by inhibiting HUWE1 in HeLa cells.
    Molecular Weight

    426.51

    Formula

    C25H26N6O
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=NC=NC(N2CCC(C3=CC=CC=C3)(C#N)CC2)=C1C)NC4=CC=C(CN)C=C4
    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 : 125 mg/mL (293.08 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 2.3446 mL 11.7231 mL 23.4461 mL
    5 mM 0.4689 mL 2.3446 mL 4.6892 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)

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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: ≥ 2.08 mg/mL (4.88 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.88 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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

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    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 +
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    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
    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 2.3446 mL 11.7231 mL 23.4461 mL 58.6153 mL
    5 mM 0.4689 mL 2.3446 mL 4.6892 mL 11.7231 mL
    10 mM 0.2345 mL 1.1723 mL 2.3446 mL 5.8615 mL
    15 mM 0.1563 mL 0.7815 mL 1.5631 mL 3.9077 mL
    20 mM 0.1172 mL 0.5862 mL 1.1723 mL 2.9308 mL
    25 mM 0.0938 mL 0.4689 mL 0.9378 mL 2.3446 mL
    30 mM 0.0782 mL 0.3908 mL 0.7815 mL 1.9538 mL
    40 mM 0.0586 mL 0.2931 mL 0.5862 mL 1.4654 mL
    50 mM 0.0469 mL 0.2345 mL 0.4689 mL 1.1723 mL
    60 mM 0.0391 mL 0.1954 mL 0.3908 mL 0.9769 mL
    80 mM 0.0293 mL 0.1465 mL 0.2931 mL 0.7327 mL
    100 mM 0.0234 mL 0.1172 mL 0.2345 mL 0.5862 mL
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    BI8622 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:

    BI86221875036-74-0BI 8622BI-8622E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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