JNK-IN-8 is a highly selective JNK inhibitor based on multiple profiling strategies. JNK-IN-8 is the first irreversible JNK inhibitor for JNK1, JNK2 and JNK4 with IC50 of 4.7 nM, 18.7 nM and 1 nM, respectively. JNK-IN-8 inhibits c-Jun phosphorylation at submicromolar concentrations in cells. JNK-IN-8 will be broadly useful as a pharmacological probe of JNK-dependent signal transduction.
|Source||Chem Biol (2012). Figure 4. JNK-IN-8|
|Cell Lines||HEK293- IL1R cells|
|Incubation Time||24 h|
|Results||JNK-IN-7, JNK-IN-8, and JNK-IN-12 exhibited only on-pathway activity as monitored by inhibition of c-Jun phosphorylation|
|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.
Discovery of potent and selective covalent inhibitors of JNK.
Zhang T, et al. Chem Biol. 2012 Jan 27;19(1):140-54. PMID: 22284361.
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