Vps34-IN-1 Property

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

form 

crystalline solid

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H332Harmful if inhaled

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Vps34-IN-1 Chemical Properties,Usage,Production

Uses

Vps34-IN-1 is a potent and selective inhibitor of phosphoinositide 3-kinase (PI3K) vacuolar protein sorting 34 (VPS34) (1). VPS34 inhibitors can be used to investigate autophagic processes (2).

Biological Activity

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 ~50-60% loss of sgk3 phosphorylation within 1 min. however, vps34-in1 could not inhibit activity of the sgk2 isoform without a ptdins(3)p-binding px domain. in addition, the combination of vps34-in1 and class i pi3k inhibitor of gdc-0941 resulted in the reduced sgk3 activity ~80-90%. therefore, these data demonstrated that vps34-in1 would be a useful probe to delineate physiological roles of the vps34 and the combination of class i such as gdc-0941 and class iii such as vps34-in1 pi3k inhibitors could be used to better analyse the roles and regulation of the elusive class ii pi3k [1].

IC 50

25 nm

References

[1] bago r et al. characterization of vps34-in1, a selective inhibitor of vps34, reveals that the phosphatidylinositol 3-phosphate-binding sgk3 protein kinase is a downstream target of class iii phosphoinositide 3-kinase. biochem j.2014 nov 1;463(3):413-27.