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BI605906

CAS No. : 960293-88-3

MCE 国际站：BI605906

产品活性：BI605906 是一种新型 IKKβ 抑制剂，在 0.1 mM ATP 条件下测定时 IC₅₀ 值为 380 nM。

研究领域：NF-κB

作用靶点：IKK

In Vitro: BI605906 is an inhibitor of IKKβ with improved selectivity. BI605906 inhibits IKKβ in vitro with an IC₅₀ value of 380 nM when assayed at 0.1 mM ATP. The only other protein kinase that is inhibited of over 100 tested, which include IKKα, IKKε and TBK1, is the insulin-like growth factor 1 (IGF1) receptor (IC₅₀=7.6 μM). BI605906 partially inhibits the IL-1-stimulated activation of IKKε/TBK1. In primary mouse hepatocytes, Metformin treatment for 3 hours suppresses TNFα-induced degradation of the NF-κB negative regulator IκB, while modulating AMPK and MTOR signaling in a dose-dependent manner. The magnitude of the effect on IκB is comparable with BI605906. Unlike Metformin, BI605906 (10 μM ) does not suppress signaling downstream of mTOR nor does it activate AMPK. TNF-α-dependent expression of CINC-1/CXCL1, CXCL2, IL-1β, and IL-6 is strongly inhibited by both Metformin and BI605906 (10 μM).

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