TAK-715

SKU: orb1301032

Description

TAK-715 is a selective small molecule inhibitor targeting the p38α MAP kinase. It has been utilized in research to investigate p38α's role in cellular stress responses and inflammation, with applications in both in vitro biochemical assays and in vivo models of inflammatory disease.

Research Area

Epigenetics & Chromatin, Metabolism Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 303162-79-0
• MW: 399.51
• Purity: 99.83% (May vary between batches)
• Formula: C₂₄H₂₁N₃OS
• SMILES: CCc1nc(c(s1)-c1ccnc(NC(=O)c2ccccc2)c1)-c1cccc(C)c1
• Target: Casein Kinase,p38 MAPK,JNK
• Solubility: Ethanol:20 mg/mL (50.06 mM);DMSO:50 mg/mL (125.15 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.01 mM)

Bioactivity

• Target IC50:
  p38β:0.20 μM|p38δ:>10 μM|p38γ:>10 μM|p38α:7.1 nM
• In Vivo:
  TAK 715 (10 mg/kg, po) inhibits LPS-induced TNF-alpha production in mice with 87.6% inhibition. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 results in Cmax of 0.19 μg/mL and AUC(0-24 hours) of 1.16 μg·h/mL in rats. TAK 715 (30 mg/kg, po) significantly reduces the secondary paw volume with 25 % inhibition in a rat adjuvant-induced arthritis (AA) model.
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• In Vitro:
  TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM. TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells. The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TAK 715, TAK1, TAK715, TAK-715, Snai1, Wnt/β-catenin, TNF-α, p38α, p38MAPK, p38δ, p38β, p38γ, p38 MAPK, orally, inhibit, JNK1, ERK1, IKKβ, MEKK1, hDvl2, Inhibitor, CYP3A4, CTGF, arthritis, CaseinKinase, Casein Kinase

Compound Identifiers

PubChem CID

9952773