S-7979 SP600125, >99%

Synonyms : [1,9-Pyrazoloanthrone] [Anthrapyrazolone] [JNK Inhibitor II] [SAPK Inhibitor II]

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  • 50 mg
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  • 100 mg
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  • 300 mg
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  • 500 mg
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  • 1 g
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  • 315
  • 273
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  • 2 g
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  • 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.
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