Takinib,1111556-37-6

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Takinib

CAS No. : 1111556-37-6

MCE 国际站：Takinib

产品活性：Takinib (EDHS-206) 是一种有效且选择性的 TAK1 抑制剂 (IC₅₀=9.5 nM)，比 IRAK4 (IC₅₀=120 nM) 和 IRAK1 (IC₅₀=390 nM) 作用强 1.5 log 倍。Takinib 是一种TAK1自磷酸化的抑制剂，在 ATP 结合口袋内非竞争性结合。在类风湿关节炎和转移性乳腺癌细胞模型中，Takinib 诱导 TNF-α 刺激的细胞凋亡 (apoptosis)。Takinib 也是恶性疟原虫蛋白激酶 9 (PfPK9) 的抑制剂 (K_D(app) of 0.46 nM)。

研究领域：MAPK/ERK Pathway  |  Apoptosis

作用靶点：MAP3K  |  Apoptosis

In Vitro: Takinib (10-10000 nM; 24 hours) induces apoptosis following TNF-α stimulation in MDA-MB-231 cells.
?Takinib (10 μM; 0-1 hours) reduces phosphorylation of IKK and p65.
?Takinib serves as a chemical starting point for the development of PfPK9 (K_D(app) of 0.46 μM) inhibitors for malaria.
?Takinib (2 hours; 0.1-20 μM; human RASFs) induces phosphorylation of TAK1^Thr184/187, STAT3^Tyr705 and STAT3^Ser727 in IL-1β-treated (10 ng/mL; 30 min) RASFs.

In Vivo: Takinib (50 mg/kg; intraperitoneally; daily from days 18-36) reduces the clinical score in type II collagen-induced arthritis (CIA) mouse model of rheumatoid arthritis.
?Takinib (50 mg/kg; oral gavage; daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice.

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