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S-7979 SP600125, >99%       Prices Reduced (November 2011)

[Anthra(1,9-cd)pyrazol-6(2H)-one] [1,9-Pyrazoloanthrone] [Anthrapyrazolone] [JNK Inhibitor II] [SAPK Inhibitor II]

M.W. 220.23

C14H8N2O

[129-56-6]

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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• 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).

  Inhibitory activity of SP600125 on various enzymes (adapted from Han, Z., et al.)

  Enzyme	IC50 (µM)		Enzyme	IC50 (µM)
  JNK1	0.11		Phospholipase A2	> 10
  JNK2	0.11		Adenylate cyclase	> 10
  JNK3	0.15		Guanylate cyclase	> 10
  ERK2	> 30		ATPase (Na/K)	> 10
  p38β	> 30		Protein kinase C	> 10
  IkB kinase-2	> 30		HIV-1 protease	> 10
  Acetylcholine esterase	> 10		Monoamine oxidase	> 10
  Cycloxygenase-2	> 10		Tyrosine hydrolase	> 10
  5'-lipoxygenase	> 10		Elastase	> 10
  PDE I, III, IV, V	> 10		Cathepsin B, G	> 10
  iNOS	> 10		EGFR tyrosine kinase	> 10

• SP600125 inhibited JNK, reduced the levels of c-Jun phosphorylation, prevented apoptosis in dopaminergic neurons, and partly reversed the loss of dopamine in MPTP-induced Parkinson's disease in C57BL/6N mice.  Wang W., et al.  "SP600125, a new JNK inhibitor, protects dopaminergic neurons in the MPTP model of Parkinson's disease."  Neurosci. Res. 48:  195-202 (2004).

• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.