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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Based on 23 publication(s) in Google Scholar

Other Forms of Takinib:

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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    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 : 2.5 mg/mL (7.76 mM; ultrasonic and warming and heat to 60°C; 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.

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    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.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.41%

    SDS (393 KB)

    COA (250 KB) HNMR (357 KB) RP-HPLC (255 KB) LCMS (129 KB)

    Handling Instructions (2659 KB)
    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
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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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