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The p90 ribosomal S6 kinases (RSK) 1-4 are downstream members of the extracellular signal-regulated kinase (ERK)/MAPK cascade. SL 0101-1 is a kaempferol glycoside, isolated from the tropical plant F. refracta, that selectively inhibits RSK2 with an IC50 value of 89 nM (Ki = 1 μM) without interfering with upstream activators of RSK, including ERK, MEK, EGFR, and PKC. At 100 μM, SL 0101-1 inhibits the proliferation of MCF-7 breast cancer cells, arresting cells in the g1 phase of the cell cycle. SL 0101-1 has been used to characterize the intracellular signaling events associated with angiotensin II-induced tyrosine kinase activation with a concentration of 30 μM attenuating angiotensin II-induced cell proliferation.
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