JNK-IN-8

• GMP format available

JNK-IN-8 is a selective and irreversible inhibitor of c-Jun N-terminal kinases (JNK1, JNK2, and JNK3). It effectively inhibits JNK activity with IC50 values of 4.7 nM, 18.7 nM, and 1 nM, respectively. JNK-IN-8 forms a covalent bond with a conserved cysteine residue in the JNK active site, leading to a conformational change that blocks substrate binding.

This compound is widely used in research to study JNK-related signaling pathways, including stress responses, apoptosis, and T cell differentiation. Its high specificity and potency make it a valuable tool for investigating the role of JNK in various cellular processes.

Key features and applications include:

• Selective and Irreversible Inhibition: JNK-IN-8 is a highly selective and irreversible inhibitor of c-Jun N-terminal kinases (JNK1, JNK2, and JNK3) with IC50 values of 4.67 nM, 18.7 nM, and 0.98 nM, respectively. In cancer research, JNK-IN-8 is used to study the role of JNK signaling in cancer cell proliferation, survival, and apoptosis.
• Covalent Binding: It forms covalent bonds with a conserved cysteine residue in the JNK enzymes, leading to a conformational change that blocks substrate binding and inhibits kinase activity.
• Specificity: JNK-IN-8 exhibits high specificity for JNK1/2/3 and does not significantly inhibit other kinases.

Relevant disease states include:

• Cancer: JNK-IN-8 has been shown to suppress tumor growth in various cancers, including triple-negative breast cancer (TNBC) and colorectal cancer.
• Inflammatory Diseases: Dysregulated JNK signaling is associated with inflammatory conditions, making JNK-IN-8 relevant in research on diseases like rheumatoid arthritis and inflammatory bowel disease.
• Neurodegenerative Diseases: JNK-IN-8 is studied for its potential in treating neurodegenerative diseases such as Alzheimer’s and Parkinson’s diseases.