TG100-115

TG100-115 is a potent small molecule PI3K γ/δ inhibitor potently inhibited edema and inflammation in response to multiple mediators known to participate in myocardial infarction, including vascular endothelial growth factor and platelet-activating factor. TG100-115, inhibited PI3Kγ and -δ (IC50 values of 83 and 235 nM, respectively), whereas both PI3Kα and -β were relatively unaffected (IC50 values >1 μM). TG100-115 also blocked histamine-induced permeability, as predicted based on PI3K's role in GPCR signaling. Additionally, TG100-115 did not block VEGF-induced angiogenesis in vivo.