2. MAPK/ERK Pathway Stem Cell/Wnt Cell Cycle/DNA Damage
  3. p38 MAPK Casein Kinase
  4. TAK-715

TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model.

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TAK-715 Chemical Structure

TAK-715 Chemical Structure

CAS No. : 303162-79-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 13 publication(s) in Google Scholar

TAK-715 Related Antibodies

Top Publications Citing Use of Products

    TAK-715 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 21;9:660.  [Abstract]

    By Western blotting, the α-SMA and palladin proteins are determined in cells that are pretreated with NF-κB (JSH-23), Wnt/β-catenin (XAV939), EGFR (erlotinib), p38 MAPK (TAK-715), and Smad3 (SIS3) inhibitors and are followed by TWEAK stimulation.

    View All p38 MAPK Isoform Specific Products:

    View All Isoforms
    p38 MAPK p38α p38β MAPK13 p38δ p38γ

    View All Casein Kinase Isoform Specific Products:

    View All Isoforms
    CK1 CK2

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model[1][2].

    IC50 & Target[1][2]

    p38α

    7.1 nM (IC50)

    p38β

    200 nM (IC50)

    p38δ

    >10 μM (IC50)

    p38γ

    >10 μM (IC50)

    CK1δ

     

    CK1ε

     

    In Vitro

    TAK-715 (compound 8h) inhibits LPS-stimulated release of TNF-α from THP-1 (IC50=48 nM) and has no inhibitory activity for major CYPs, including CYP3A4. TAK-715 has no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1 (IC50>10 μM of all)[1].
    TAK 715 (10 μM; 1 hour) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells[2].
    TAK-715 (1 μM; pretreatment for 16 hours) dramatically suppresses Norepinephrine (NE)-stimulated induction of fibronectin, CTGF, and Snai1 expression in TGF-β1-treated HK-2 cells at both the mRNA and protein levels[3].

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

    TAK-715 Related Antibodies
    In Vivo

    TAK-715 (compound 8h; 3-30 mg/kg; PO) significantly reduces the secondary paw volume[1].
    TAK-715 (10 mg/kg; PO) has a Cmax of 0.19 μg/mL and an AUC of 1.16 μg h/mL.

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

    Animal Model: 7-week-old male Lewis rats with arthritis[1]
    Dosage: 3, 10, 30 mg/kg
    Administration: PO; single dose
    Result: Significantly reduced the secondary paw volume (25% inhibition)
    Animal Model: Rat[1]
    Dosage: 10 mg/kg (Pharmacokinetic Analysis)
    Administration: PO
    Result: Had a Cmax of 0.19 μg/mL and an AUC of 1.16 μg•h/mL.
    Clinical Trial
    Molecular Weight

    399.51

    Formula

    C24H21N3OS
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC=CC=C1)NC2=NC=CC(C3=C(N=C(S3)CC)C4=CC=CC(C)=C4)=C2
    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 : ≥ 100 mg/mL (250.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5031 mL 12.5153 mL 25.0307 mL
    5 mM 0.5006 mL 2.5031 mL 5.0061 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: ≥ 2.5 mg/mL (6.26 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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 (6.26 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (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

    Purity: 99.76%

    COA (254 KB) LCMS (94 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, 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 2.5031 mL 12.5153 mL 25.0307 mL 62.5767 mL
    5 mM 0.5006 mL 2.5031 mL 5.0061 mL 12.5153 mL
    10 mM 0.2503 mL 1.2515 mL 2.5031 mL 6.2577 mL
    15 mM 0.1669 mL 0.8344 mL 1.6687 mL 4.1718 mL
    20 mM 0.1252 mL 0.6258 mL 1.2515 mL 3.1288 mL
    25 mM 0.1001 mL 0.5006 mL 1.0012 mL 2.5031 mL
    30 mM 0.0834 mL 0.4172 mL 0.8344 mL 2.0859 mL
    40 mM 0.0626 mL 0.3129 mL 0.6258 mL 1.5644 mL
    50 mM 0.0501 mL 0.2503 mL 0.5006 mL 1.2515 mL
    60 mM 0.0417 mL 0.2086 mL 0.4172 mL 1.0429 mL
    80 mM 0.0313 mL 0.1564 mL 0.3129 mL 0.7822 mL
    100 mM 0.0250 mL 0.1252 mL 0.2503 mL 0.6258 mL
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    TAK-715 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:

    TAK-715303162-79-0TAK715TAK 715p38 MAPKCasein KinaseorallyWnt/β-cateninarthritisTNF-αCYP3A4JNK1ERK1IKKβMEKK1TAK1hDvl2CTGFSnai1Inhibitorinhibitorinhibit

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