1. NF-κB
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  3. B022

B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor (Ki of 4.2 nM; IC50=15.1 nM). B022 protects liver from toxin-induced inflammation, oxidative stress, and injury. B022 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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B022 Chemical Structure

B022 Chemical Structure

CAS No. : 1202764-53-1

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Solid + Solvent
10 mM * 1 mL in DMSO
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    B022 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Dec 16;13(1):7782.  [Abstract]

    B022 (5 µM; 48 h) significantly attenuates MLN-induced aberrant NIK signaling in HepG2 cells. Veh (black), B022 (blue).

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    • Biological Activity

    • Purity & Documentation

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    • Customer Review

    Description

    B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor (Ki of 4.2 nM; IC50=15.1 nM). B022 protects liver from toxin-induced inflammation, oxidative stress, and injury[1][2]. B022 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

    IC50 & Target

    Ki: 4.2 nM (NF-κB-inducing kinase (NIK))[1]

    In Vitro

    B022 (0-5 μM; 12 hours; Hepa1 cells) treatment suppresses NIK-induced p52 formation in a dose-dependent manner[1].
    ? B022 (0-5 μM; 12 hours; Hepa1 cells) treatment for 8 h completely blocks NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5[1].
    ? B022 prevents NIK- or H2O2-induced β cell death and also ameliorates streptozotocin (STZ)-induced β cell death and hyperglycemia[3].

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

    Western Blot Analysis[1]

    Cell Line: Hepa1 cells
    Concentration: 0 μM, 0.5 μM, 5 μM
    Incubation Time: 12 hours
    Result: Suppressed NIK-induced p52 formation in a dose-dependent manner.

    RT-PCR[1]

    Cell Line: Hepa1 cells
    Concentration: 0 μM, 0.5 μM, 5 μM
    Incubation Time: 12 hours
    Result: Dose-dependently blocked NIK-induced expression of chemokines, cytokines, and iNOS in these cells. Completely blocked NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5.
    In Vivo

    B022 (30 mg/kg; intravenous injection; twice a day; for 10 days; STOP-NIK male mice) treatment inhibits NIK-triggered liver inflammation and injury in STOP-NIK mice infected with cre adenoviruses[1].

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

    Animal Model: STOP-NIK male mice (8 weeks) infected with Ad-cre[1]
    Dosage: 30 mg/kg
    Administration: Intravenous injection; twice a day; for 10 days
    Result: Completely prevents the lethal effect of abnormally high levels of hepatic NIK in mice. Inhibited the majority of the deteriorating effects of aberrant activation of hepatic NIK.
    Molecular Weight

    397.88

    Formula

    C19H16ClN5OS

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CC(C1=NC=CS1)(C#CC2=CC3=C(CCN3C4=NC(N)=NC=C4Cl)C=C2)O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 250 mg/mL (628.33 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 2.5133 mL 12.5666 mL 25.1332 mL
    5 mM 0.5027 mL 2.5133 mL 5.0266 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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 (5.23 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% Corn Oil

      Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    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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    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5133 mL 12.5666 mL 25.1332 mL 62.8330 mL
    5 mM 0.5027 mL 2.5133 mL 5.0266 mL 12.5666 mL
    10 mM 0.2513 mL 1.2567 mL 2.5133 mL 6.2833 mL
    15 mM 0.1676 mL 0.8378 mL 1.6755 mL 4.1889 mL
    20 mM 0.1257 mL 0.6283 mL 1.2567 mL 3.1417 mL
    25 mM 0.1005 mL 0.5027 mL 1.0053 mL 2.5133 mL
    30 mM 0.0838 mL 0.4189 mL 0.8378 mL 2.0944 mL
    40 mM 0.0628 mL 0.3142 mL 0.6283 mL 1.5708 mL
    50 mM 0.0503 mL 0.2513 mL 0.5027 mL 1.2567 mL
    60 mM 0.0419 mL 0.2094 mL 0.4189 mL 1.0472 mL
    80 mM 0.0314 mL 0.1571 mL 0.3142 mL 0.7854 mL
    100 mM 0.0251 mL 0.1257 mL 0.2513 mL 0.6283 mL
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    B022 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.

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    Product Name:
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    Cat. No.:
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