2. MAPK/ERK Pathway Apoptosis
  3. MAP3K Apoptosis
  4. Takinib

Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM).

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Takinib Chemical Structure

Takinib Chemical Structure

CAS No. : 1111556-37-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 57 In-stock
Solid
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5 mg USD 80 In-stock
10 mg USD 150 In-stock
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Customer Review

Based on 19 publication(s) in Google Scholar

Takinib Related Antibodies

Top Publications Citing Use of Products

    Takinib purchased from MedChemExpress. Usage Cited in: Mol Biol Cell. 2018 Oct 1;29(20):2470-2480.  [Abstract]

    WT and WDR62-KO cells are pre-incubated withTakinib (2 µM) for 1 h then treated with TNFα (50 ng/mL) for 15 min. JNK activation is determined by Western blotting.

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    MAP3K7/TAK1 MAP3K8 ASK2 MAP3K5/ASK1

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    Description

    Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM)[1][2][3].

    IC50 & Target[1]

    TAK1

    9.5 nM (IC50)

    IRAK4

    120 nM (IC50)

    IRAK1

    390 nM (IC50)

    GCK

    430 nM (IC50)

    CLK2

    430 nM (IC50)

    MINK1

    1.9 μM (IC50)

    In Vitro

    Takinib (10-10000 nM; 24 hours) induces apoptosis following TNF-α stimulation in MDA-MB-231 cells[1].
    Takinib (10 μM; 0-1 hours) reduces phosphorylation of IKK and p65[1].
    Takinib serves as a chemical starting point for the development of PfPK9 (KD(app) of 0.46 μM) inhibitors for malaria[3].
    Takinib (2 hours; 0.1-20 μM; human RASFs) induces phosphorylation of TAK1Thr184/187, STAT3Tyr705 and STAT3Ser727 in IL-1β-treated (10 ng/mL; 30 min) RASFs[4].

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

    Takinib Related Antibodies

    Western Blot Analysis[1]

    Cell Line: Breast cancer cell line MDA-MB-231
    Concentration: 10 μM
    Incubation Time: 5, 15, 30, 60 minutes
    Result: IKK and p65 were maximally phosphorylated at 15 minutes, which indicated activation of the NF-κB pathway, while p38 phosphorylation peaks at 30 minutes.

    Western Blot Analysis[4]

    Cell Line: IL-1β-treated (10 ng/mL; 30 min) RASFs
    Concentration: 0.1-20 µM
    Incubation Time: 2 hours
    Result: Induced phosphorylation of TAK1Thr184/187, STAT3Tyr705 and STAT3Ser727.
    In Vivo

    Takinib (50 mg/kg; intraperitoneally; daily from days 18-36) reduces the clinical score in type II collagen-induced arthritis (CIA) mouse model of rheumatoid arthritis[4].
    Takinib (50 mg/kg; oral gavage; daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice[5].

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

    Animal Model: Male DBA/1 mice (CIA arthritis model)[4]
    Dosage: 50 mg/kg
    Administration: Intraperitoneally; daily from days 18-36
    Result: Showed a reduction in clinical arthritic score compared to vehicle control.
    Animal Model: Female NSG mice (8 weeks old)[5]
    Dosage: 50 mg/kg
    Administration: Oral gavage; daily until 17 days
    Result: Slowed tumor growth and reduced tumor size/weight.
    Molecular Weight

    322.36

    Formula

    C18H18N4O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CCCN1C2=CC=CC=C2N=C1NC(C3=CC(C(N)=O)=CC=C3)=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 : 50 mg/mL (155.11 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 3.1021 mL 15.5106 mL 31.0212 mL
    5 mM 0.6204 mL 3.1021 mL 6.2042 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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    Volume (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: 2.5 mg/mL (7.76 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 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 (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 (7.76 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 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 (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

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    (per animal)

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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 +
    % 
    +
    %
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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, 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 3.1021 mL 15.5106 mL 31.0212 mL 77.5530 mL
    5 mM 0.6204 mL 3.1021 mL 6.2042 mL 15.5106 mL
    10 mM 0.3102 mL 1.5511 mL 3.1021 mL 7.7553 mL
    15 mM 0.2068 mL 1.0340 mL 2.0681 mL 5.1702 mL
    20 mM 0.1551 mL 0.7755 mL 1.5511 mL 3.8777 mL
    25 mM 0.1241 mL 0.6204 mL 1.2408 mL 3.1021 mL
    30 mM 0.1034 mL 0.5170 mL 1.0340 mL 2.5851 mL
    40 mM 0.0776 mL 0.3878 mL 0.7755 mL 1.9388 mL
    50 mM 0.0620 mL 0.3102 mL 0.6204 mL 1.5511 mL
    60 mM 0.0517 mL 0.2585 mL 0.5170 mL 1.2926 mL
    80 mM 0.0388 mL 0.1939 mL 0.3878 mL 0.9694 mL
    100 mM 0.0310 mL 0.1551 mL 0.3102 mL 0.7755 mL
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    Takinib 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:

    Takinib1111556-37-6EDHS-206EDHS206EDHS 206MAP3KApoptosisMAP kinase kinase kinase, MEKK, MAPKKKcancerarthritismalariaRA-FLSMDA-MB-231HepG2HuH7RASFInhibitorinhibitorinhibit

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