SP600125 **

产品名称：SP600125
产品货号：LC  S-7979
产品规格：100 MG
Novel, potent and selective JNK-1,-2, and -3 inhibitor (Ki = 0.19 µM).  SP600125 is an ATP-competitive reversible inhibitor with >20-fold selectivity vs. a range of kinases and enzymes tested.  In cells, SP600125 caused a dose-dependent inhibition of the phosphorylation of c-Jun, the expression of inflammatory genes IL-2, COX-2, TNF-α, IFN-γ, and blocked the activation and differentiation of primary human CD4 cell cultures.  In animal studies, SP600125 inhibited bacterial lipopolysaccharide-induced expression of tumor necrosis factor-α and prevented anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes.  Bennett, B.L., et al.  "SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase."  Proc. Natl. Acad. Sci. USA 98:  13681-13686 (2001).
SP600125 completely inhibited IL-1-induced accumulation of phospho-Jun and initiation of c-Jun transcription in synoviocytes.  Han, Z., et al.  "c-Jun N-terminal kinase is required for metalloproteinase expression and joint destruction in inflammatory arthritis."  J. Clin. Invest. 108:  73-81 (2001).
Storage:  Store at or below -20 ºC.  Solubility:  Prepare initial stock solutions in DMSO (soluble at 65 mg/mL) for in vitro use; solubility in ethanol or water is low.  Disposal:  A

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