SL 0101-1 is a selective p90 ribosomal S6 kinase (RSK) inhibitor for RSK2 with an IC50 of 89 nM. The IC50 of kaempferol, the flavonoid constituent of SL 0101-1, is 15 μM for RSK. The rhamnose moiety of SL 0101-1 increases the affinity for RSK by >150-fold. Purified SL 0101-1 is specific for inhibition of RSK activity compared with that of p70 S6K and MSK1.SL 0101-1 exhibits selective and potent p90 Rsk inhibitory activity at nanomolar concentrations without inhibiting the function of upstream kinases such as MEK, Raf, or PKC. Prevention of RSK by SL 0101-1 could occur through interaction with either the NTKD or the CTKD. SL 0101-1 effectively inhibits the isolated RSK2 NTKD. SL 0101-1 is much less effective in suppressing the mutant in comparison with wild-type RSK2 or wild-type RSK1. Additionally, prevention of RSK by SL 0101-1 occurs through competition with ATP for the nucleotide-binding site of the NTKD and further attests to the specificity of SL 0101-1. SL 0101-1 is membrane permeable and is effective in intact cells. SL 0101-1 does not affect the phosphorylation of RSK2. SL 0101-1 inhibits proliferation of the MCF-7 line with an efficacy paralleling its ability to inhibit RSK in intact cells but has no effect on the growth of the normal breast cell line MCF-10A. SL 0101-1 is not toxic and preferentially inhibits the growth of the breast cancer cell line relative to that of the normal breast cell line.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
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