Sunday 10 December 2023 - 21:54
NOTE: our usual phone and fax lines are down, due to a dispute between our landlord and Verizon.
In the meantime, please use this mobile phone number: 978-715-9327 and this fax number: 781-415-0695
The 25% Discount for Shopping Cart Purchases is now PERMANENT !!
For Online Shopping Cart Orders Only
In-Stock Sizes Only
See Check-out Page For Further Details
FREE SHIPPING TO THE U.S. AND 32 OTHER COUNTRIES! [Read more].
S-7979 SP600125, >99%
Synonyms : [1,9-Pyrazoloanthrone] [Anthrapyrazolone] [JNK Inhibitor II] [SAPK Inhibitor II]
- Size
- US $
- €
- £
- ¥
- 50 mg
- 48
- 44
- 38
- 7,000
- In stock
- 100 mg
- 86
- 79
- 68
- 12,500
- In stock
- 300 mg
- 135
- 125
- 107
- 19,600
- In stock
- 500 mg
- 186
- 172
- 148
- 26,900
- In stock
- 1 g
- 334
- 309
- 266
- 48,400
- In stock
- 2 g
- 495
- 459
- 394
- 71,700
- In stock
Note: Our Euro, Pound, and Yen prices are revised regularly to account for currency exchange rate fluctuations.
- 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.
- 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.