SP600125

SP6000125 is a pan-inhibitor of JNK (IC50s = 0.04, 0.04, and 0.09 µM for JNK1, -2, and -3, respectively). 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-1beta, IL-8, and TNF-alpha in isolated human peripheral blood monocytes, as well as decreases anti-CD3- and anti-CD28-induced production of IFN-gamma, TNF-alpha, 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. 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.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: 220.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 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.