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Ki= 57 μM

BGP-15 is a PARP inhibitor.

As a group of pharmacological inhibitors of the enzyme poly ADP ribose polymerase(PARP), PARP inhibitors are considered a potential treatment for stroke and myocardial infarction.

In vitro: Previous study showed that BGP-15 at 200 μM could prevent the imatinib-induced oxidative damages, attenuate the depletion of high-energy phosphates, alter the signaling effect of imatinib by preventing p38 MAP kinase and JNK activation, and also induce the Akt and GSK-3β phosphorylation [1].

In vivo: In-vivo study indicated that BGP-15 improved cardiac function and reduced arrhythmic episodes in two HF and AF mouse models. In these models, BGP-15 was associated with increased phosphorylation of IGF1R. Moreover, cardiac-specific IGF1R transgenic overexpression in mice recapitulated the protection caused by BGP-15. The authors further demonstrated that BGP-15 with IGF1R could provide protection independent of phosphoinositide 3-kinase-Akt and heat-shock protein 70 [2].

Clinical trial: A safety and efficacy of BGP-15 in patients with type 2 diabetes mellitus has been scheduled, however, this study is now terminated due to the funding support withdrawn

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