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Submit ReviewTakinib 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. 了解 Tocris 化合物库的更多信息。
分子量 | 322.37 |
公式 | C18H18N4O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1111556-37-6 |
PubChem ID | 37750349 |
InChI Key | UOZVVPXKJGOFIG-UHFFFAOYSA-N |
Smiles | CCCN1C(NC(C2=CC(C(N)=O)=CC=C2)=O)=NC3=CC=CC=C13 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 32.24 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for Takinib, please let us know.
关键词: 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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