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SP 600125 JNK1/2/3 inhibitor

Catalog No.A4604
Size Price Stock Qty
10mM (in 1mL DMSO)
$55.00
In stock
SP600125 Evaluation Sample
$28.00
In stock
10mg
$50.00
In stock
50mg
$65.00
In stock
100mg
$85.00
In stock

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Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Wang Y, Li Y, et al. "The cerebral cavernous malformation disease causing gene KRIT1 participates in intestinal epithelial barrier maintenance and regulation." FASEB J. 2018 Sep 25:fj201800343R. PMID:30252535
2. MXinwei Feng1, Junfeng Lu2, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.
3. Sharma K, Vu TT, et al. "p53-independent Noxa induction by cisplatin is regulated by ATF3/ATF4 in head and neck squamous cell carcinoma cells." Mol Oncol. 2018 Jan 19. PMID:29352505
4. He GR, Lin XK, et al. "Dexmedetomidine impairs Pglycoprotein mediated efflux function in L02 cells via the denosine5'monophosphate activated protein kinase/nuclear factor κB pathway." Mol Med Rep. 2018 Apr;17(4):5049-5056. PMID:29393492

Quality Control

Chemical structure

SP 600125

Related Biological Data

SP 600125

Related Biological Data

SP 600125

Related Biological Data

SP 600125

Related Biological Data

SP 600125

Biological Activity

Description SP600125 is a broad-spectrum inhibitor of JNK for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM, respectively.
Targets JNK1 JNK2 JNK3 Aurora A Flt3 TRKA
IC50 40 nM 40 nM 90 nM 60 nM 90 nM 70 nM

Protocol

Cell experiment: [1]

Cell lines

MIN6 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

40 μM, 36 hours

Applications

When the MIN6 cells were transfected with the Gal4 plasmid and CREB plasmid, SP600125 significantly stimulated CREB-mediated promoter activity in a dose-dependent manner. There was a 2.8-fold increase in this reporter activity after exposure of the transfected MIN6 cells to 20 μM of the inhibitor.

Animal experiment: [2]

Animal models

Female C57BL/6 mice

Dosage form

Subcutaneous injection; 15 mg/kg; administered at 0, 12, 24, and 36 h

Applications

Anti-CD3 (50 μg) i.p. was administered as a single dose immediately after SP600125 at time 0. After 48 h, mice were killed, and the thymus was dissected for thymocyte isolation. Mice receiving SP600125 showed almost complete resistance to CD3 Ab-mediated apoptosis with CD4+CD8+ numbers the same as control animals.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Vaishnav D, Jambal P, Reusch J E B, et al. SP600125, an inhibitor of c-jun N-terminal kinase, activates CREB by a p38 MAPK-mediated pathway. Biochemical and biophysical research communications, 2003, 307(4): 855-860.

[2] Bennett B L, Sasaki D T, Murray B W, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proceedings of the National Academy of Sciences, 2001, 98(24): 13681-13686.

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Chemical Properties

Cas No. 129-56-6 SDF Download SDF
Synonyms N/A
Chemical Name dibenzo[cd,g]indazol-6(2H)-one
Canonical SMILES O=C1C2=CC=CC3=C2C(C4=CC=CC=C41)=NN3
Formula C14H8N2O M.Wt 220.23
Solubility ≥11mg/mL in DMSO Storage Desiccate at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

SP600125 is a selective, reversible and ATP-competitive inhibitor of Jun N-terminal kinase (JNK) with IC50 values of 40, 40 and 90 nM for JNK1, 2 and 3, respectively [1].

SP600125 was screened out from a time-resolved f luorescence assay using the GST-c-Jun and recombinant human JNK2. In this assay, SP600125 showed a Ki value of 190 nM. SP600125 was also found to inhibit JNK1, 2 and 3 isoforms in the selectivity tests. The selectivity of SP600125 for JNK is 300-fold greater than that for ERK1 and p38-2. In Jurkat T cells, SP600125 suppressed the phosphorylation of c-Jun with IC50 of 5-10 μM. SP600125 also inhibited the expression of IL-2 and IFN-γ in cells stimulated with PMA and phytohemagglutinin, since JNK had been reported to regulate the transcription of IL-2. Besides that, SP600125 exerted differential inhibition of cytokines in CD4+ cells as well as inflammatory genes in monocytes. Moreover, SP600125 administration significantly inhibited TNF-α expression induced by LPS in a mouse model, suggesting that it had efficacy in endotoxin-induced inf lammation in vivo [1].

References:
[1] Bennett B L, Sasaki D T, Murray B W, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proceedings of the National Academy of Sciences, 2001, 98(24): 13681-13686.