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JNK-IN-8 (JNK Inhibitor XVI) is a potent JNK inhibitor with IC50s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, 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.
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Source | Chem Biol (2012). Figure 4. JNK-IN-8 |
| Method | Western Blot | |
| Cell Lines | HEK293- IL1R cells | |
| Concentrations | 1.0 μM | |
| 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 |
| Cell Experiment | |
|---|---|
| Cell lines | MDA-MB-436 and HCC1569 cell lines |
| Preparation method | Cells were plated at 40% confluency in 96-well, flat bottom plates. After being allowed to attach overnight, cells were treated with vehicle JNK-IN-8, lapatinib, or JNK-IN-8 and lapatinib combination for various timepoints. After treatment, MTT was added to a final concentration of 0.5mg/ml from 5mg/ml stock in PBS. Cellular metabolism reduces this tetrazole to insoluble formazan crystals. After four hours of incubation, the media + MTT was gently removed. Formazan crystals were dissolved using DMSO and absorbance at 590nm was read. |
| Concentrations | 5 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | MDA-MB-231 xenograft nude mice |
| Formulation | - |
| Dosages | 25mg/kg/day |
| Administration | Intraperitoneal injection |
| Molecular Weight | 507.59 |
| Formula | C29H29N7O2 |
| CAS Number | 1410880-22-6 |
| Solubility (25°C) | DMSO ≥ 35 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Zhang T, et al. Chem Biol. Discovery of potent and selective covalent inhibitors of JNK.
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