Cited by 2,558Protein Kinase Regulation and GTPase SignalingNF-κB Signaling PathwaysMelanoma and MAPK Pathways

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SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase

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Bennett, Brydon L., Sasaki, Dennis T., Murray, Brion W., O'Leary, Eoin C., Sakata, Steve T., Xu, Weiming, Leisten, Jim C., Motiwala, Aparna, Pierce, Steve, Satoh, Yoshitaka, Bhagwat, Shripad S., Manning, Anthony M., Anderson, David W.·2001·Proceedings of the National Academy of Sciences

DOI 10.1073/pnas.251194298PMC PMC61101

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Abstract

Jun N-terminal kinase (JNK) is a stress-activated protein kinase that can be induced by inflammatory cytokines, bacterial endotoxin, osmotic shock, UV radiation, and hypoxia. We report the identification of an anthrapyrazolone series with significant inhibition of JNK1, -2, and -3 ( K i = 0.19 μM). SP600125 is a reversible ATP-competitive inhibitor with >20-fold selectivity vs. a range of kinases and enzymes tested. In cells, SP600125 dose dependently inhibited the phosphorylation of c-Jun, the expression of inflammatory genes COX-2 , IL-2 , IFN -γ, TNF -α, and prevented the activation and differentiation of primary human CD4 cell cultures. In animal studies, SP600125 blocked (bacterial) lipopolysaccharide-induced expression of tumor necrosis factor-α and inhibited anti-CD3-induced apoptosis of CD4 + CD8 + thymocytes. Our study supports targeting JNK as an important strategy in inflammatory disease, apoptotic cell death, and cancer.

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Authors: Bennett, B. L., Sasaki, D. T., Murray, B. W., O'Leary, E. C., Sakata, S. T., Xu, W., Leisten, J. C., Motiwala, A., Pierce, S., Satoh, Y., Bhagwat, S. S., Manning, A. M., & Anderson, D. W.
Affiliations: Signal Research Division, Celgene Corporation, 5555 Oberlin Drive, San Diego, CA 92121
Yale University (US)
ORCID: Bennett, Brydon L.
Murray, Brion W.
Manning, Anthony M.
Anderson, David W.
Venue: Proceedings of the National Academy of Sciences
Publisher: National Academy of Sciences
Published: 2001-11-20
Volume: 98
Issue: 24
Pages: 13681-13686
ISSN: 0027-8424 (ISSN-L)
1091-6490
DOI: 10.1073/pnas.251194298
PMC: PMC61101
OpenAlex: W2096931514
Cited by: 2,558
References: 46
Citations by year: 2026: 40 · 2025: 49 · 2024: 77 · 2023: 66 · 2022: 51 · 2021: 69 · 2020: 71 · 2019: 52 · 2018: 60 · 2017: 91 · 2016: 97 · 2015: 80 · 2014: 100 · 2013: 107 · 2012: 132
FWCI: 47.43
Type: journal article
Language: en
Open access: green
europepmc.org
Locations: Proceedings of the National Academy of Sciences (publishedVersion)
Europe PMC (PubMed Central) (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › NF-κB Signaling Pathways
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Melanoma and MAPK Pathways
Keywords: SP600125, Jun N-terminal kinase, ATP-competitive kinase inhibitors, c-Jun phosphorylation, inflammatory gene expression, cyclooxygenase-2, TNF-α, lipopolysaccharide, CD4+ T cell activation, apoptosis, thymocytes, inflammatory diseases, cancer
MeSH terms: Adenosine Triphosphate, Animals, Anthracenes, Anthraquinones, Binding, Competitive, Cell Differentiation, Cells, Cultured, Enzyme Inhibitors, Female, Humans, Lymphocyte Activation, Mice, Inbred C57BL, Monocytes, Pyrazoles, Structure-Activity Relationship, Tumor Necrosis Factor-alpha, Molecular Structure, CD4-Positive T-Lymphocytes, Gene Expression, Cytokines, Jurkat Cells, Mitogen-Activated Protein Kinases, Pyrazolones, Protein Kinase Inhibitors, JNK Mitogen-Activated Protein Kinases, Mice

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SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase

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