1. NF-κB
  2. IKK
  3. BI605906

BI605906 is a novel IKKβ inhibitor with an IC50 value of 380 nM when assayed at 0.1 mM ATP.

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

BI605906 Chemical Structure

BI605906 Chemical Structure

CAS No. : 960293-88-3

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mg USD 160 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    BI605906 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2017 Jun 1;66(5):698-710.e5.  [Abstract]

    Western blot analysis of cell lysates from primary MEFs using the indicated antibodies. Cells are pre-treated with IKK2i (BI605906, 10 μM) for 1 hr, followed by stimulation with TNF (10 ng/mL) for the indicated times.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BI605906 is a novel IKKβ inhibitor with an IC50 value of 380 nM when assayed at 0.1 mM ATP.

    IC50 & Target[1]

    IKKβ

    380 nM (IC50, at 0.1 mM ATP)

    In Vitro

    BI605906 is an inhibitor of IKKβ with improved selectivity. BI605906 inhibits IKKβ in vitro with an IC50 value of 380 nM when assayed at 0.1 mM ATP. The only other protein kinase that is inhibited of over 100 tested, which include IKKα, IKKε and TBK1, is the insulin-like growth factor 1 (IGF1) receptor (IC50=7.6 μM). BI605906 partially inhibits the IL-1-stimulated activation of IKKε/TBK1[1]. In primary mouse hepatocytes, Metformin treatment for 3 hours suppresses TNFα-induced degradation of the NF-κB negative regulator IκB, while modulating AMPK and MTOR signaling in a dose-dependent manner. The magnitude of the effect on IκB is comparable with BI605906. Unlike Metformin, BI605906 (10 μM ) does not suppress signaling downstream of mTOR nor does it activate AMPK. TNF-α-dependent expression of CINC-1/CXCL1, CXCL2, IL-1β, and IL-6 is strongly inhibited by both Metformin and BI605906 (10 μM)[2].

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

    Molecular Weight

    432.51

    Formula

    C17H22F2N4O3S2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=C(N)C2=C(C(F)(F)CC)C=C(N3CCC(S(=O)(C)=O)CC3)N=C2S1)N

    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 (115.60 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 2.3121 mL 11.5604 mL 23.1209 mL
    5 mM 0.4624 mL 2.3121 mL 4.6242 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: ≥ 1.25 mg/mL (2.89 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: 1.25 mg/mL (2.89 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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).
    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: 99.70%

    References
    Cell Assay
    [2]

    Primary hepatocytes are incubated in serum-free medium overnight and then stimulated for 3 h with or without 2 mM Metformin and TNF-α. In addition, cells are incubated with/without 10 μM BI605906 or 100 nM Rapamycin, before lysis and immunoblotting[2].

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

    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 2.3121 mL 11.5604 mL 23.1209 mL 57.8021 mL
    5 mM 0.4624 mL 2.3121 mL 4.6242 mL 11.5604 mL
    10 mM 0.2312 mL 1.1560 mL 2.3121 mL 5.7802 mL
    15 mM 0.1541 mL 0.7707 mL 1.5414 mL 3.8535 mL
    20 mM 0.1156 mL 0.5780 mL 1.1560 mL 2.8901 mL
    25 mM 0.0925 mL 0.4624 mL 0.9248 mL 2.3121 mL
    30 mM 0.0771 mL 0.3853 mL 0.7707 mL 1.9267 mL
    40 mM 0.0578 mL 0.2890 mL 0.5780 mL 1.4451 mL
    50 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1560 mL
    60 mM 0.0385 mL 0.1927 mL 0.3853 mL 0.9634 mL
    80 mM 0.0289 mL 0.1445 mL 0.2890 mL 0.7225 mL
    100 mM 0.0231 mL 0.1156 mL 0.2312 mL 0.5780 mL
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    BI605906 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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