CAS NO: | 960293-88-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | BI605906 is a novelIKKβinhibitor with anIC50value of 380 nM when assayed at 0.1 mM ATP. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | BI605906 is an inhibitor of IKKβ with improved selectivity. BI605906 inhibits IKKβ in vitro with an IC50value 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[1]. 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)[2]. | ||||||||||||||||
分子量 | 432.51 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C17H22F2N4O3S2 | ||||||||||||||||
CAS 号 | 960293-88-3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(115.60 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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