NF-κB is important in regulating cellular responses because it belongs to the category of "rapid-acting" primary transcription factors, i.e., transcription factors that are present in cells in an inactive state and do not require new protein synthesis in order to become activated (other members of this family include transcription factors such as c-Jun, STATs, and nuclear hormone receptors). This allows NF-κB to be a first responder to harmful cellular stimuli. Known inducers of NF-κB activity are highly variable and include reactive oxygen species (ROS), tumor necrosis factor alpha (TNFα), interleukin 1-beta (IL-1β), bacterial lipopolysaccharides (LPS), isoproterenol, cocaine, and ionizing radiation.
Vemurafenib (PLX4032, RG7204)是一种新型有效的B-RafV600E抑制剂,IC50为31 nM。
MoreIsoprenaline hydrochloride是非选择性的β-肾上腺素受体激动剂,与肾上腺素相似。
MoreDoxazosin mesylate能选择性拮抗突触后的α1肾上腺素受体。
MoreBI-D1870是ATP竞争性S6核糖体抑制剂,对RSK1/2/3/4的IC50分别为31 nM/24 nM/18 nM/15 nM,比对MST2,GSK-3β,MARK3,CK1 和Aurora B的抑制性高10到100倍。
MorePF-4708671是一种可渗透细胞的p70 S6K1亚型抑制剂,Ki/IC50为20 nM/160 nM,作用于S6K1比作用于S6K2选择性高400倍,作用于S6K1比作用于MSK1和RSK1/2选择性分别高4和20倍以上,是第一个报道的S6K1特异性抑制剂。
MoreVemurafenib (PLX4032, RG7204)是一种新型有效的B-RafV600E抑制剂,IC50为31 nM。
MoreIsoprenaline hydrochloride是非选择性的β-肾上腺素受体激动剂,与肾上腺素相似。
MoreDoxazosin mesylate能选择性拮抗突触后的α1肾上腺素受体。
MoreBI-D1870是ATP竞争性S6核糖体抑制剂,对RSK1/2/3/4的IC50分别为31 nM/24 nM/18 nM/15 nM,比对MST2,GSK-3β,MARK3,CK1 和Aurora B的抑制性高10到100倍。
MorePF-4708671是一种可渗透细胞的p70 S6K1亚型抑制剂,Ki/IC50为20 nM/160 nM,作用于S6K1比作用于S6K2选择性高400倍,作用于S6K1比作用于MSK1和RSK1/2选择性分别高4和20倍以上,是第一个报道的S6K1特异性抑制剂。
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