1. MAPK/ERK Pathway
  2. MAP3K

Takinib 

Cat. No.: HY-103490 Purity: 98.00%
Handling Instructions

Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM.

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

Takinib Chemical Structure

Takinib Chemical Structure

CAS No. : 1111556-37-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
1 mg USD 80 In-stock
Estimated Time of Arrival: December 31
5 mg USD 140 In-stock
Estimated Time of Arrival: December 31
10 mg USD 220 In-stock
Estimated Time of Arrival: December 31
50 mg USD 880 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

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

    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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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM.

    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

    At 10 mM, Takinib shows significant inhibitory activity (<10% enzyme activity after exposure) on six serine/threonine kinases, including TAK1, IRAK4, IRAK1, GCK, CLK2, and MINK1. Analysis reveals that increasing concentrations of Takinib leads to a decrease in Vmax while maintaining KM. When the enzyme is activated with 5 mM ATP for 3 hr, the same Vmax is reached for 0, 10, 50, and 100 nM Takinib, and KM increases for these concentrations, which implies that Takinib is an ATP-competitive inhibitor if TAK1 is ATP activated. Importantly, results show that Takinib inhibits the function of both activated and un-activated TAK1 with identical potency. TNF-α stimulation in the presence of Takinib induces caspase activity in MDA-MB-231 cells in a dose-dependent manner, whereas unstimulated cells do not upregulate caspase activity. Takinib reduces phosphorylation significantly but does not influence total protein levels. Takinib inhibits phosphorylation of IKK, MAPK 8/9, and c-Jun in a dose-dependent manner. Takinib shows an almost complete inhibition of IL-6 secretion at micromolar concentrations following 24 hr of treatment in the presence of TNF-α[1].

    Solvent & Solubility
    In Vitro: 

    DMSO : 6.8 mg/mL (21.09 mM; Need ultrasonic and warming)

    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
    10 mM 0.3102 mL 1.5511 mL 3.1021 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    Activity of purified TAK1-TAB1 protein is measured. In brief, TAK1-TAB1 (50 ng/well) is incubated with 5 μM ATP containing radiolabeled [32P]-ATP in the presence of 300 mM substrate peptide (RLGRDKYKTLRQIRQ) in a final volume of 40 μL in the presence of buffer (containing 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% β-Mercaptoethanol, 10 mM magnesium acetate, 0.5 mM MnCl) and indicated compounds. The reaction is let go for 10 min and stopped with 10 μL concentrated H3PO4. The remaining activity is measured using a scintillation counter. Dose-response curves are repeated 3 times. For kinetic mechanistic studies, experiments are repeated two times and averaged[1].

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

    Cell Assay
    [1]

    MDA-MB-231 cells (1,000 cells/well) are seeded in a 96-well plate with 10% FBS, 5% Pen/Strep, 4 g/L glucose DMEM medium. After 24h, cells are serum starved with 1% FBS, 5% Pen/Strep, 4 g/L glucose DMEM medium for 4h. Cells are treated with titrations of Takinib in the presence or absence of 30 ng/mL TNFα. Plates at 0 h and 24 h following treatment are frozen at -80°C after removal of media. After 24 h, 100 μL ddH2O is added to each well and plates are refrozen. 1 μL from Hoechst stock [1 mg/mL in 1:4 DMSO/H2O] is dissolved in 1 mL of TNE buffer (10 mM Tris, 2 M NaCl, 1 mM Na2EDTA) and 100 μL of this solution is added to each well. The fluorescence is determined at 355/460 nm[1].

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

    References
    Molecular Weight

    322.36

    Formula

    C₁₈H₁₈N₄O₂

    CAS No.

    1111556-37-6

    SMILES

    CCCN1C2=CC=CC=C2N=C1NC(C3=CC(C(N)=O)=CC=C3)=O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    Cat. No.:
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    Takinib

    Cat. No.: HY-103490