Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM. Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1).
IC50&Target
RSK2
~5.5 μM (IC50)
Nrf2
Human Endogenous Metabolite
体外研究
It is showed that carnosol has no cytotoxic effects on GES1 cells and 10 μM carnosol strongly suppresses RSK2 activity, but has little effect on any other kinase. Carnosol exerts strong dose-dependent inhibitory effects against RSK2 autophosphorylation and phosphorylation of its substrate ATF1.
体内研究
Results indicate that Carnosol significantly decreaseS the volume and weight of gastric tumors relative to the vehicle-treated group. Additionally, mice tolerate treatment with carnosol without significant loss of body weight similar to the vehicle-treated group. The phosphorylation of CREB, a direct downstream protein of RSK2, Is strongly inhibited in the carnosol-treated group but the expression of total CREB is relatively unchanged.
分子式
C20H26O4
分子量
330.42
CAS号
5957-80-2
中文名称
鼠尾草酚
运输条件
Room temperature in continental US; may vary elsewhere.