SP600125,
>99%
[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] | RTECS: CB4585000 |
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
View the MSDS for this product
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, veterinary, food, or household use
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