AZD6482 is a potent, selective and ATP competitive PI3Kβ inhibitor (IC(50) 0.01 μm). AZD6482 inhibited insulin-induced human adipocyte glucose uptake in vitro (IC(50) of 4.4 μm). This is the first human target validation for PI3Kβ inhibition as anti-platelet therapy showing a mild and generalized antiplatelet effect attenuating but not completely inhibiting multiple signaling pathways with an impressive separation towards primary hemostasis. AZD6482 at 'supratherapeutic' plasma concentrations may attenuate insulin signaling, most likely through PI3Kα inhibition.
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PKI-402; Voxtalisib; Pilaralisib; PI-3065; VS-5584; PIK-294; GSK1059615; AZD8186; CUDC-907; AZD8835; AMG319; Buparlisib hydrochloride; Umbralisib; PIK-III; VPS34-IN1; VPS34 inhibitor 1; Wortmannin