TG100-115

TG100-115 inhibited PI3Kγ and PI3K&delta, (IC50 values of 83 and 235 nM, respectively), whereas both PI3Kα and PI3Kβ were relatively unaffected (IC50 values >1 µ M). In 133 protein kinase panel, TG100-115 did not show significant inhibition (IC50 values >1 µ M). In a mouse murine asthma model, TG100-115 markedly reduced the pulmonary eosinophilia and the concomitant interleukin-13 and mucin accumulation. TG100-115 also inhibited inflammatory patterns in mouse smoke model. In a rat and porcine model of myocardial infraction TG100-115 potently inhibited edema and inflammation in response to multiple mediators, including vascular endothelial growth factor and platelet-activating factor. By contrast, endothelial cell mitogenesis, a repair process important to tissue survival after ischemic damage, was not disrupted.

677297-51-7

C₁₈H₁₄N₆O₂

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