SP 600125 , an anthrapyrazolone inhibitor of Jun N-terminal kinase

  title={SP 600125 , an anthrapyrazolone inhibitor of Jun N-terminal kinase},
  author={Brydon L. Bennett and Dennis T. Sasaki and Brion William Murray and Eoin C. O’Leary and Steve T. Sakata and Weiming Xu and Jim C. Leisten and Aparna Motiwala and Steve Pierce and Yoshitaka Satoh and Shripad S. Bhagwat and Anthony M. Manning and David W. Anderson},
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 (Ki 0.19 M). SP600125 is a reversible ATPcompetitive 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… CONTINUE READING
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