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VPS34-IN-1 | VPS34-IN-1 : Inhibitor of PIK3C3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PIK3C3
  • IC50:28 nM
  • IC50:25 nM
  • Activity:~20% remaining
Inhibitor
from 100 nM up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Protein kinase profiling of the VPS34-IN1 at a single concentration of 1 μM carried out against the ...

Potency
Cellular
In Vitro

PIK3C3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1042/BJ20140889

Orthogonal Probes def

PICTILISIB

Chemical Information

Molecular Formula C21H24ClN7O
SMILEs CC(C)(O)CNc1ncc(-c2ccnc(Nc3ccnc(Cl)c3)n2)c(CC2CC2)n1
InChI InChI=1S/C21H24ClN7O/c1-21(2,30)12-26-19-25-11-15(17(29-19)9-13-3-4-13)16-6-8-24-20(28-16)27-14-5-7-23-18(22)10-14/h5-8,10-11,13,30H,3-4,9,12H2,1-2H3,(H,25,26,29)(H,23,24,27,28)
Molecular weight 425.17 Da
AlogP 3.8609000000000018
HBond acceptors 8
HBond donors 3
Atoms 54

References

Publications

Cross References

canSARChEMBLBindingDB

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Expert Reviews

by SERP
(on 30 Oct 2024)
Cellular Use Rating
Direct target engagement in cells has not been demonstrated.
by SERP
(on 20 Feb 2025)
Cellular Use Rating
VPS34-IN-1 is a moderately potent (25nM biochemical, 0.1-1uM cellular) and very selective kinase inhibitor. It shows 50-fold or more selectivity against other lipid kinases, and a very clean profile in...
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