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

TAK-715 

Cat. No.: HY-10456 Purity: 99.89%
Handling Instructions

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.

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

TAK-715 Chemical Structure

TAK-715 Chemical Structure

CAS No. : 303162-79-0

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 396 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    TAK-715 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jun 21;9:660.

    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.

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    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].

    In Vivo

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

    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.

    303162-79-0

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (250.31 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" 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
    10 mM 0.2503 mL 1.2515 mL 2.5031 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    TAK-715TAK715TAK 715p38 MAPKCasein KinaseorallyWnt/β-cateninarthritisTNF-αCYP3A4JNK1ERK1IKKβMEKK1TAK1hDvl2CTGFSnai1Inhibitorinhibitorinhibit

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    Product Name:
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