SP 600125 is a potent and reversible inhibitor of JNK1-3 with an IC50 value of 0.11 ?M.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. SP 600125 also prevents apoptosis in many cell types, including B-cells, and inhibits autophagy in HeLa cells. Competitively and reversibly inhibits JNK1, 2 and 3 (IC50 = 40 - 90 nM) with negligible activity at ERK2, p38β and a range of enzymes (IC50 > 10 ?M). Active in vivo. Shown to have reduced selectivity over other protein kinases under certain conditions. Protects renal tubular epithelial cells against ischemia/reperfusion-induced apoptosis. Prevents BMP9-induced osteogenic differentiation of MSCs.
Bennett, B.L, et al. SP600125, an anthrapyrazolone inhibitor of jun N-terminal kinase.Proc Natl Acad Sci USA.,2001,98 (24), 13681-13686.
Kim, Y.S., 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 Immunol.,2008,1816158-6169.
Hazard Statements: H315-H319-H335
Causes skin irritation. Causes serious eye irritation. May cause respiratory irritation.
Precautionary Statements: P261-P264b-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P332+P313-P337+P313-P362-P501c
Avoid breathing dust/fume/gas/mist/vapours/spray. Wash face, hands and any exposed skin thoroughly after handling Use only outdoors or in a well-ventilated area. Wear protective gloves/protective clothing/eye protection/face protection. IF ON SKIN: Wash with plenty of soap and water. IF INHALED: Remove to fresh air and keep at rest in a position comfortable for breathing. IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. Call a POISON CENTER or doctor/physician if you feel unwell. If skin irritation occurs: Get medical advice/attention. If eye irritation persists: Take off contaminated clothing and wash before reuse. Dispose of contents/ container to an approved waste disposal plant