Selective
inhibitor of c-Jun N-terminal kinase (JNK). 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 μM). Active in vivo. Shown to have
reduced selectivity over other protein kinases under certain conditions.
Protects renal tubular epithelial cells against ischaemia/reperfusion-induced
apoptosis.
Bennettet al (2001) SP600125, an anthrapyrazolone
inhibitor of Jun N-terminal kinase. Proc.Natl.Acad.Sci.USA 98 13681.
Schnablet al (2001) TAK1/JNK and p38 have opposite
effects on rat hepatic stellate cells. Hepatology 34 953. Bain
et al (2003) The specificities of protein kinase inhibitors: an
update. Biochem.J. 371 199. Wanget al (2007)
SP600125, a selective JNK inhibitor, protects ischemic renal injury via
suppressing the extrinsic pathways of apoptosis. Life Sci. 80
2067.
“Tocris is to be congratulated for continuing to meet the current demand for a rapid and reliable source of high-quality compounds that are urgently needed as pharmacological tools by a growing international population of cannabinoid researchers..”
