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. 2018 Feb 6;9(76):34200–34212. doi: 10.18632/oncotarget.24409

Figure 2. Carnosol is a potent RSK2 inhibitor.

Figure 2

(A) Screening ofthe effect of carnosol on various kinases. The effect of carnosol on kinase activity of DNA-PK, MEK1, TOPK, ERK2, RSK2, PI3K (p110α/p65α), PI3-K (p110α/p85α), PI3-K (p110β/p85α), PI3-K (p110γ/p85α), PDK1, AKT1, AKT2, GSK3β or mTOR was determined using active kinases and the specific substrate for each kinase. (B) Effect of carnosol on EGF-induced activation of various signaling proteins in JB6 cells. Serum-starved (0.1% FBS; 24 h) JB6 cells were treated with various doses of carnosol for 1.5 h followed by treatment with EGF for 30 min. (C) Effect of carnosol on various signaling proteins in SGC7901 gastric cancer cells. Cells were treated with carnosol at 20 or 40 μM for 3 h and then signaling pathway proteins were examined by Western blotting. (D) Carnosol suppresses RSK2 kinase activity in a dose-dependent manner. The effect of carnosol on RSK2 activity was assessed by an in vitro kinase assay using RSK2 (active, 300 ng) and ATF1 (substrate, 300 ng) proteins. The effect of carnosol on RSK2 activity was determined by Western blotting. For (B–D) data, similar results were obtained from 3 independent experiments.