| Identification | Back Directory | [Name]
Vps34-IN-1 | [CAS]
1383716-33-3 | [Synonyms]
CS-2377
Vps34-IN-1
1-[[2-[(2-Chloro-4-pyridinyl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino]-2-methyl-2-propanol
1-((2-((2-chloropyridin-4-yl)amino)-4'-(cyclopropylmethyl)-[4,5'-bipyrimidin]-2'-yl)amino)-2-methylpropan-2-ol
2-Propanol, 1-[[2-[(2-chloro-4-pyridinyl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino]-2-methyl- | [Molecular Formula]
C21H24ClN7O | [MDL Number]
MFCD28963905 | [MOL File]
1383716-33-3.mol | [Molecular Weight]
425.91 |
| Hazard Information | Back Directory | [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. |
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Musechem
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+1-800-259-7612 |
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www.musechem.com |
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