SP600125 A potent, selective and reversible inhibitor of JNK1, JNK-2, and JNK-3

SP600125 (CAS 129-56-6)

SP600125 | CAS 129-56-6 is rated 5.0 out of 5 by 3.
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Synonym: JNK Inhibitor II; Anthra(1,9-cd)pyrazol-6(2H)-one
Application: A potent, selective and reversible inhibitor of JNK1, JNK-2, and JNK-3
CAS Number: 129-56-6
Purity: ≥97%
Molecular Weight: 220.23
Molecular Formula: C14H8N2O
* Refer to Certificate of Analysis for lot specific data (including water content).
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SP600125 is a potent, selective and reversible inhibitor of the three JNK enzymes (c-Jun N-terminal kinases), with IC50 = 40 nM for JNK1 and JNK2, and 90 nM for JNK3. Inhibition is competitive with respect to ATP, and over 300-fold more selective for JNK as compared to ERK1 and p38-2 MAP kinases. SP600125 was shown to cause a dose-dependent inhibition of the phosphorylation of c-Jun, and thereby the expression of inflammatory genes COX-2, IFN-γ, IL-2, TNF-α, and block the activation and differentiation of primary human CD4 cell cultures. SP 600125 has also been shown to prevent apoptosis in an array of cell types, and inhibit autophagy in HeLa cells.


References

1. Bennett, B.L., et al. 2001. Proc. Natl. Acad. Sci. U.S.A. 98: 13681-13686. PMID: 11717429
2. Han, Z., et al. 2001. J. Clin. Invest. 108: 73-81. PMID: 11435459
3. Wang, W., et al. 2004. Neurosci. Res. 48: 195-202. PMID: 14741394
4. Kim, Y.S., et al. 2008. J Immunol. 181: 6158-6169. PMID: 18941206

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in water (partly ), DMSO (100 mM), ethanol (5 mM), and methanol.
Storage :
Store at room temperature
Melting Point :
283° C
Boiling Point :
~489.3° C at 760 mmHg (Predicted)
Density :
~1.5 g/cm3 (Predicted)
Refractive Index :
n20D 1.80 (Predicted)
IC50 :
JNK1: IC50 = 40 nM; JNK2: IC50 = 40 nM; JNK3: IC50 = 90 nM; PKR: IC50 = 8 µM (human)
pK Values :
pKa: 11.75 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
CB4585000
PubChem CID :
8515
MDL Number :
MFCD00022289
EC Number :
204-955-6
SMILES :
C1=CC=C2C(=C1)C3=NNC4=CC=CC(=C43)C2=O

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Certificate of Analysis

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SP600125  Product Citations

See how others have used SP600125. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 116 total

PMID: # 28753407  Hosokawa, Y. et al. 2017. Immunol. Invest. 46: 615-624.

PMID: # 28598976  Mukherjee, S. et al. 2017. PLoS ONE. 12: e0179203.

PMID: # 28299790  Choi, M. et al. 2017. Br. J. Pharmacol. 174: 1810-1825.

PMID: # 28190264  Ocaña, GJ. et al. 2017. Immunology. 151: 198-210.

PMID: # 28383550  Wassermann-Dozorets, R. et al. 2017. Cell Death Dis. 8: e2733.

PMID: # 28327651  Hsieh, MJ. et al. 2017. Sci Rep. 7: 45039.

PMID: # 28499910  Aseer, KR. et al. 2017. Free Radic. Biol. Med. 108: 874-895.

PMID: # 27357344  Ardura, JA. et al. 2017. Journal of cellular physiology. 232: 785-796.

PMID: # 28414095  Waetzig, V. et al. 2017. Mol. Cell. Neurosci. 82: 12-22.

PMID: # 28656053  Liang, RN. et al. 2017. Evid Based Complement Alternat Med. 2017: 6489427.

Citations 1 to 10 of 116 total

How long can this product be stored in a DMSO solution?

Asked by: SCM4
Thank you for your question. Long term storage at -20 ºC in DMSO is acceptable for this product.
Answered by: Technical Support
Date published: 2017-03-27

Any recommendations for solubility in DMSO?

Asked by: chemicalsmg
The solubility of SP600125 is 100 mM in DMSO. We recommend rapid stirring, sonication or gentle warming (in a 45-60°C water bath).
Answered by: Tech Service 11
Date published: 2017-03-06
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Rated 5 out of 5 by from works well! Good in lower concentration; higher concentration significantly inhibits Erk signalling. Long lasting inhibition of JNK – checked up to 24 hrs.
Date published: 2017-02-07
Rated 5 out of 5 by from We used this in different human cell lines We used this in different human cell lines and got good results.
Date published: 2015-10-16
Rated 5 out of 5 by from HepG2 HepG2, Hep3B and PLC/PRF/5 cells were pre-treated with SP600125 (from SCBT) before exposure to galangin in order to further characterize galangin's involvement in endoplasmic reticulum stress.
Date published: 2015-02-27
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