BIX 02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM. BIX 02189 inhibited catalytic function of purified, MEK5 enzyme. The MEK5 inhibitors blocked phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. BIX 02189 also inhibited transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade, in a cellular trans-reporter assay system.
|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.
|Solubility||DMSO 50 mg/mL
Ethanol 50 mg/mL
|Source||Sci Rep (2018). Figure 3. BIX 02189|
|Method||cell proliferation assay|
|Cell Lines||colorectal cancer cells|
|Concentrations||100 nM to 30 μM|
|Incubation Time||24 or 48 h|
|Results||The data suggested that doses of BIX02189 that completely inhibited ERK5 signaling had no effect on cell proliferation|
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