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GSK2830371 | GSK2830371 : Allosteric inhibitor of Wip1
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PPM1D
  • IC50:6 nM
  • IC50:13 nM
  • INH:100 -1000 nM
Allosteric
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
GSK2830371 was tested for inhibition of biochemical activity against a panel of 21 phosphatases (Mil ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Tested against various hematological cell lines

Potency
Cellular
In Vitro

PPM1D

Mode of Action: Allosteric

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/nchembio.1427

In Vivo Validations

Mouse
Dose: 150 mg/Kg
Route of delivery: Oral
Plasma half life: short half-life

DOI Reference: 10.1038/nchembio.1427

Chemical Information

Molecular Formula C23H29ClN4O2S
SMILEs Cc1ncc(Cl)cc1NCc1ccc(C(=O)N[C@@H](CC2CCCC2)C(=O)NC2CC2)s1
InChI InChI=1S/C23H29ClN4O2S/c1-14-19(11-16(24)12-25-14)26-13-18-8-9-21(31-18)23(30)28-20(10-15-4-2-3-5-15)22(29)27-17-6-7-17/h8-9,11-12,15,17,20,26H,2-7,10,13H2,1H3,(H,27,29)(H,28,30)/t20-/m0/s1
Molecular weight 460.17 Da
AlogP 0.0
HBond acceptors 6
HBond donors 3
Atoms 60

Vendors

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Expert Reviews

by SERP
(on 21 Feb 2023)
Cellular Use Rating
In Model Organisms
Proteomic analysis (Silac) with GW2830371 and inactive analog 10 (same chemotype) in ref 10.1038/NCHEMBIO.1427 identified Wip1 as primary target.
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