TOPK-p38 JNK-IN-1 (Compound B12) is an orally active inhibitor of the TOPK-p38 JNK signaling pathway, with an IC50 value of 2.14 μM for the inhibition of NO production. It demonstrates anti-inflammatory properties by inhibiting downstream phosphorylation of related proteins and preventing the degradation of TOPK [1].
OTS964 is a potent, orally active compound that operates as a highly selective inhibitor of TOPK with an IC 50 of 28 nM [1]. Additionally, it demonstrates significant inhibitory action against cyclin-dependent kinase CDK11, specifically binding to CDK11B with a K d of 40 nM [2].
ADA-07 is a TOPK inhibitor which interacts with TOPK at the ATP-binding pocket and inhibits its kinase activity, thereby suppressing SUV-induced phosphorylation of ERK1 2, p38, and JNKs, and subsequently inhibiting AP-1 activity.