Description
SP600125 is a reversible ATP-competitive inhibitor which can inhibit JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM.
In vitro
SP600125 is a reversible ATP-competitive inhibitor which can inhibit JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM. SP600125 dose dependently inhibited the phosphorylation of c-Jun, the expression of inflammatory genes COX-2, IL-2, IFN-gamma, TNF-alpha, and prevented the activation and differentiation of primary human CD4 cell cultures. SP600125 is ATP-competitive (Ki=33 uM) but noncompetitive with substrate, GST-ATF2. SP600125 shows 10-fold selectivity (MKK4), 25-fold selectivity (MKK3, MKK6, PKB, and PKC-alpha),and 100-fold selectivity for other kinases. SP600125 blocks JNK and not other inflammatory-signaling cascades, and seems to have a selectivity of at least 10-fold for the JNK pathway.
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