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The three isoforms of c-Jun N-terminal kinase (JNK) are members of the MAP kinase superfamily that induce the expression of immediate-early genes in response to specific stress and inflammatory signals. Through these actions, the JNK enzymes modulate cell proliferation, apoptosis, differentiation, and autophagy. SP 600125 is a potent and reversible inhibitor of JNK1, 2, and 3, with an IC50 value of 0.11 μM.1 It is cell-permeable and dose-dependently inhibits c-Jun phosphorylation in cells, blocking the expression of COX-2 and TNF-α in monocytes and IL-10, TNF-α, and IFN-γ in T-cells.1 SP 600125 also prevents apoptosis in many cell types, including B-cells,2 and inhibits autophagy in HeLa cells.3
1
Bennett, B.L., Sasaki, D.T., Murray, B.W., et al. SP600125, an anthrapyrazolone inhibitor of jun N-terminal kinase. Proc Natl Acad Sci USA98(24)13681-13686(2001).
2
Kim, Y.S., Park, G.B., Lee, H., et al. Cross-linking of B7-H1 on EBV-transformed B cells induces apoptosis through reactive oxygen species production, JNK signaling activation, and fasL expression. J Immunol1816158-6169(2008).
3
Zhang, Y., Wu, Y., Cheng, Y., et al. Fas-mediated autophagy requires JNK activation in HeLa cells. Biochem Biophys Res Commun3771205-1210(2008).
Synonyms
1PMV
Pyrazolanthrone
NSC 75890
Formal Name
anthra[1,9-cd]pyrazol-6(2H)-one
CAS Number
129-56-6
Molecular Formula
C14H8N2O
Formula Weight
220.2
Formulation
A crystalline solid
Purity
≥98%
Stability
2 years
Storage
-20°C
Shipping
Room temperature
in continental US; may vary elsewhere
SMILES
Copy SMILES to clipboard
O=c1c2ccccc2c2n[nH]c3cccc1c23
Background Reading
Bennett, B.L., Sasaki, D.T., Murray, B.W., et al. SP600125, an anthrapyrazolone inhibitor of jun N-terminal kinase. Proc Natl Acad Sci USA98(24)13681-13686(2001).
Lawrence, M.C., Jivan, A., Shao, C., et al. The roles of MAPKs in disease. Cell Res18436-442(2008).
Zhang, Y., Wu, Y., Cheng, Y., et al. Fas-mediated autophagy requires JNK activation in HeLa cells. Biochem Biophys Res Commun3771205-1210(2008).
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5 mg
$37.00
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10 mg
$70.00
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25 mg
$167.00
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50 mg
$296.00
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