Product Introduction
Bioactivity


英文名: BI605906

描述: BI605906 is an inhibitor of IKKβ. When assayed at 0.1 mM ATP, the IC50 value is 380 nM.

体外活性: BI605906 is an inhibitor of IKKβ with improved selectivity. BI605906 partially inhibits the IL-1-stimulated activation of IKKε/TBK1[1]. 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). TNF-α-dependent expression of CINC-1/CXCL1, CXCL2, IL-1β, and IL-6 is strongly inhibited by both Metformin and BI605906 (10 μM)[2]. 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (231.21 mM)


关键字: BI605906 | BI 605906 | BI-605906

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