VPS34-IN1 is a potent and selective Vps34 inhibitor with potential anticancer activity. VPS34-IN1 inhibits Vps34 with 25 nM IC50 in vitro, but does not significantly inhibit the activity of 340 protein kinases or 25 lipid kinases tested that include all isoforms of class I as well as class II PI3Ks. Administration of VPS34-IN1 to cells induces a rapid dose-dependent dispersal of a specific PtdIns(3)P-binding probe from endosome membranes, within 1 min, without affecting the ability of class I PI3K to regulate Akt. Combining class I (GDC-0941) and class III (VPS34-IN1) PI3K inhibitors could be used as a strategy to better analyse the roles and regulation of the elusive class II PI3K.
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PKI-402; Voxtalisib; Pilaralisib; PI-3065; VS-5584; PIK-294; AZD6482; GSK1059615; AZD8186; CUDC-907; AZD8835; AMG319; Buparlisib hydrochloride; Umbralisib; PIK-III; VPS34 inhibitor 1; Wortmannin