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Biological Activity:
Potent and specific inhibitor of the p90 ribosomal S6 kinase (RSK) isoforms in vitro and in vivo, which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro with an IC50 of 10–30 nM.
References:
GP Sapkota et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem. J. 2007, 401, 29–38. [online]
TL Nguyen. Targeting RSK: An Overview of Small Molecule Inhibitors. Anti-Cancer Agents Med. Chem. 2008, 8, 710-716. [online]
R Zaru et al. The MAPK-activated kinase Rsk controls an acute Toll-like receptor signaling response in dendritic cells and is activated through two distinct pathways. Nature Immunology 2007, 8, 1227 - 1235. [abstract] [Figure 2]
Chemical Name: 2-(3,5-Difluoro-4-hydroxy-phenylamino)-5,7-dimethyl-8-(3-methyl-butyl)-7,8-dihydro-5H-pteridin-6-one
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