A pan-JNK inhibitor
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SP600125

Item No. 10010466

Technical Information
Formal Name
anthra[1,9-cd]pyrazol-6(2H)-one
CAS Number
129-56-6
Synonyms
  • C.I. 70300
  • JNK Inhibitor II
  • c-Jun N-terminal Kinase Inhibitor II
  • NSC 75890
  • 1PMV
  • Pyrazolanthrone
  • 1,9-Pyrazoloanthrone
Molecular Formula
C14H8N2O
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.3 mg/mlEthanol: 0.5 mg/ml
λmax
230, 265, 300, 336, 399 nm
SMILES
O=c1c2ccccc2c2n[nH]c3cccc1c23
InChi Code
InChI=1S/C14H8N2O/c17-14-9-5-2-1-4-8(9)13-12-10(14)6-3-7-11(12)15-16-13/h1-7H,(H,15,16)
InChi Key
ACPOUJIDANTYHO-UHFFFAOYSA-N
Origin
Synthetic
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    SP6000125 is a pan-inhibitor of JNK (IC50s = 0.04, 0.04, and 0.09 µM for JNK1, -2, and -3, respectively).1 It is greater than 300-fold selective for these enzymes over a panel of 17 additional kinases at 10 µM. SP6000125 reduces LPS-induced production of IL-1β, IL-8, and TNF-α in isolated human peripheral blood monocytes, as well as decreases anti-CD3- and anti-CD28-induced production of IFN-γ, TNF-α, and IL-10 induced by in Th1-polarized Jurkat cells, in a concentration-dependent manner. It inhibits LPS-induced production of reactive oxygen species (ROS) in, and NETosis of, isolated human neutrophils when used at a concentration of 10 µM.2 Intracerebroventricular administration of SP6000125 (30 µg/animal) prevents neuronal death in the CA1 region of the hippocampus in a rat model of transient global ischemia-reperfusion injury induced by four-vessel occlusion.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bennett, B.L., Sasaki, D.T., Murray, B.W., et alSP600125, an anthrapyrazolone inhibitor of jun N-terminal kinase. Proc. Natl. Acad. Sci. USA 98(24), 13681-13686 (2001).

    2. Khan, M.A., Farahvash, A., Douda, D.N., et alJNK activation turns on LPS- and gram-negative bacteria-induced NADPH oxidase-dependent suicidal NETosis. Sci. Rep. 7(1), 3409 (2017).

    3. Guan, Q.-H., Pei, D.-S., Zhang, Q.-G., et alThe neuroprotective action of SP600125, a new inhibitor of JNK, on transient brain ischemia/reperfusion-induced neuronal death in rat hippocampal CA1 via nuclear and non-nuclear pathways. Brain Res. 1035(1), 51-59 (2005).

    Product Citations

    Li, Z., Mbah, N.E., Overmeyer, J.H., et alThe JNK signaling pathway plays a key role in methuosis (non-apoptotic cell death) induced by MOMIPP in glioblastoma. BMC Cancer 19(1), 77 (2019).

    West, C.E., and Silverman, N. p38b and JAK-STAT signaling protect against Invertebrate iridescent virus 6 infection in Drosophila. PLoS Pathog. 14(5):e1007020, (2018).

    Zhao, X., Guo, Y., Jiang, C., et alJNK1 negatively controls antifungal innate immunity by suppressing CD23 expression. Nat. Med. 23(3), 337-346 (2017).

    Singh, S.R., Zeng, X., Zhao, J., et alThe lipolysis pathway sustains normal and transformed stem cells in adult Drosophila. Nature 538(7623), 109-113 (2016).

    d'Alencon, C.A., Peña, O.A., Wittmann, C., et alA high-throughput chemically induced inflammation assay in zebrafish. BMC Biol. 8, 151 (2010).

    Tsukui, D., Kimura, Y., and Kono, H. GM-CSF receptor/SYK/JNK/FOXO1/CD11c signaling promotes atherosclerosis. iScience 26(8), 107293 (2023).