L-JNKI-1 is a cell-permeable peptide inhibitor specific for JNK. L-JNKI-1 has been shown to effectively inhibit JNK activity in in vivo studies. It is shown that Ang II induces a dose-dependent pressor response, which was significantly attenuated by JNK inhibition. It is also found that 10 μM L-JNKI-1 decreases phosphorylated c-Jun by 98% and phosphorylated Elk-1 by 100%.
|Solubility (25°C)||Water 100 mg/mL|
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
 Che-Wei Liu, et al. Neuroreport. Stroke injury induced by distal middle cerebral artery occlusion is resistant to N-methyl-d-aspartate receptor antagonism in FVB/NJ mice
 Osvaldo Mirante, et al. Int J Mol Sci. Endogenous protease nexin-1 protects against cerebral ischemia
 Neil A Turner, et al. Int J Biochem Cell Biol. Human cardiac fibroblasts express ICAM-1, E-selectin and CXC chemokines in response to proinflammatory cytokine stimulation
 E Esneault, et al. Neuroscience. D-JNKi, a peptide inhibitor of c-Jun N-terminal kinase, promotes functional recovery after transient focal cerebral ischemia in rats
 A Fornoni, et al. Diabetologia. Inhibition of c-jun N terminal kinase (JNK) improves functional beta cell mass in human islets and leads to AKT and glycogen synthase kinase-3 (GSK-3) phosphorylation
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L-JNKI-1 is a cell-permeable peptide inhibitor specific for JNK.
Juglanin, a natural occurring flavonoid, is a JNK acticator, with inflammation and anti-tumor activities. Juglanin can induce apoptosis and autophagy on human breast cancer cells.
JNK-IN-7 is a potent JNK inhibitor with IC50 of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, respectively.
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