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.
Dichiarazioni di rischio (UE): H315-H319-H335
Causes skin irritation. Causes serious eye irritation. May cause respiratory irritation.
Dichiarazioni precauzionali: P261-P280a-P305+P351+P338-P304+P340-P405-P501a
Avoid breathing dust/fume/gas/mist/vapours/spray. Wear protective gloves and eye/face protection. IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. IF INHALED: Remove to fresh air and keep at rest in a position comfortable for breathing. Store locked up. Dispose of contents/container in accordance with local/regional/national/international regulations.