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Takinib is a potent and selective TAK1/MAP3K7 kinase inhibitor (IC50 = 8.2-9.5 nM). Selective for TAK1 over IRAK4, IRAK1, GCK, CLK2 and MINK1 (IC50 values = 120, 390, 430, 430 and 1900 nM, respectively). Demonstrates weak inhibition at Src and Yes1. Exhibits no inhibition of MAP2K or other MAP3K family members. Induces apoptosis following TNF-α stimulation in in vitro models of rheumatoid arthritis and metastatic breast cancer.
Takinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 322.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.1 mL||15.51 mL||31.02 mL|
|5 mM||0.62 mL||3.1 mL||6.2 mL|
|10 mM||0.31 mL||1.55 mL||3.1 mL|
|50 mM||0.06 mL||0.31 mL||0.62 mL|
References are publications that support the biological activity of the product.
Totzke et al (2017) Takinib, a selective TAK1 inhibitor, broadens the therapeutic efficacy of TNF-α inhibition for cancer and autoimmune disease. Cell Chem.Biol. 24 1029 PMID: 28820959
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Keywords: Takinib, Takinib supplier, Potent, selective, TAK1, MAP3K7, kinase, inhibitors, inhibits, rheumatoid, arthritis, TGFbeta, TGFβ, activated, kinases, TGFb, Other, Kinases, 6430, Tocris Bioscience
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