Background:

IC50: 25 nM

VPS34-IN1 is a Vps34 inhibitor.

The vacuolar protein sorting 34 (Vps34) class III phosphoinositide 3-kinase (PI3K) phosphorylates phosphatidylinositol (PtdIns) to generate PtdIns(3)P that regulates membrane trafficking processes through its ability to recruit a subset of proteins possessing PtdIns(3)P-binding phox homology (PX) and FYVE domains.

In vitro: VPS34-IN1 was identified to be able to inhibit in-vitro Vps34, but did not significantly inhibit the activity of tested 340 protein kinases or 25 lipid kinases that include all isoforms of class I and class II PI3Ks. Treatment of VPS34-IN1 to cells dose-dependently induced a quick dispersal of a specific PtdIns(3)P-binding probe, without altering the ability of class I PI3K to regulate Akt. Moreover, VPS34-IN1 could also induce a quick