Chemical Probes logo
GSK583 | GSK583 : ATP competitive inhibitor of RIPK2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
RIPK2
  • IC50:5 nM
  • IC50:237 nM
  • IC50:133 nM
  • IC50:18 nM
ATP competitive
200 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - RIPK3 16 nM

Potency Assay Off-Target:
RIPK3: A fluorescent polarization based binding assay was developed to quantitate interaction of no ...
Selectivity Assessment Description:
hERG: Electrophysiology; Whole cell voltage clamp technique permits investigation of the physiolo ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Cellular selectivity of GSK583 was evaluated in primary human monocytes. In the presence of 1 μM GSK ...

Potency
Cellular
In Vitro

RIPK2

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.6b00211

In Vivo Validations

Rat, Mouse
Dose: 2 mg/kg oral, 1 mg/kg IV crossover (mouse and rat)
Route of delivery: Intravenous, Oral
Plasma half life: 3.1 h (rat), 2.1 h (mouse)
Systemic clearance: 15 mL/min/kg (rat), 13 mL/min/kg (mouse)

DOI Reference: 10.1021/acs.jmedchem.6b00211

Chemical Information

Molecular Formula C20H19FN4O2S
SMILEs CC(C)(C)S(=O)(=O)c1ccc2nccc(Nc3n[nH]c4ccc(F)cc34)c2c1
InChI InChI=1S/C20H19FN4O2S/c1-20(2,3)28(26,27)13-5-7-16-14(11-13)17(8-9-22-16)23-19-15-10-12(21)4-6-18(15)24-25-19/h4-11H,1-3H3,(H2,22,23,24,25)
Molecular weight 398.12 Da
AlogP 4.566000000000003
HBond acceptors 6
HBond donors 2
Atoms 47

References

Publications

Cross References

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 17 Mar 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 27 Mar 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 29 Mar 2017 )
Cellular Use Rating
In Model Organisms
GSK583 is a potent and selective molecule for the inhibition of RIP2 kinase, and it could be useful in probing the role of NOD1 and NOD2 in the pathogenesis of inflammatory disease. The compound has...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria