Drug intelligence / Profile preview

SP-600125

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

SP-600125 is a potent, selective, and reversible small molecule inhibitor of c-Jun N-terminal kinase (JNK). It acts as an ATP-competitive antagonist, targeting all three JNK isoforms (JNK1, JNK2, and JNK3) with similar potency. Originally developed by Signal Pharmaceuticals (later acquired by Celgene and subsequently Bristol Myers Squibb), the compound is widely utilized in biomedical research to investigate the role of the JNK signaling pathway in various physiological and pathological processes, including apoptosis, inflammation, and insulin resistance. In preclinical studies, SP-600125 has demonstrated the ability to reduce the phosphorylation of c-Jun and inhibit the production of inflammatory mediators like TNF-alpha. While it has shown efficacy in animal models of diabetes, rheumatoid arthritis, and neurodegenerative diseases, its use remains largely confined to the laboratory setting as a pharmacological tool due to concerns regarding specificity and potential off-target effects in clinical applications.

Other names
1,9-pyrazoloanthroneanthrapyrazolone
02

Targets

AHR (Aryl hydrocarbon receptor)JNK (Mitogen-activated protein kinase kinase kinase family)NTRK1 (Tropomyosin-related receptor kinase A)AURKA (Aurora kinase A)TTK (TTK protein kinase)MELK (Maternal embryonic leucine zipper kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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