TK-129 is an orally active, potent inhibitor of KDM5B with IC 50 of 44 nM that is low-toxicity. TK-129 shows cardioprotective effects by inhibiting KDM5B and blocking the KDM5B -associated Wnt pathway. TK-129 can be used in cardiovascular disease studies which reduce isoprenaline-induced myocardial remodelling and fibrosis in vivo as well as reduce ang II-induced activation of cardiac fibroblasts in vitro [1].