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Skepinone-L | Skepinone-L : ATP competitive inhibitor of MAPK14
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
MAPK14
  • Kd:1.5 nM
  • IC50:5 nM
  • IC50:40 nM
  • IC50:25 nM
ATP competitive
100-400 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
In a panel of 402 kinases at 1 uM, no notable activity was detected other than for p38 MAPK alpha an ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Skepinone-L did not affect phosphorylation of c-Jun or CREB.

Potency
Cellular
In Vitro

MAPK14

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.761

In Vivo Validations

Mouse
Dose:
Route of delivery: Oral

DOI Reference: 10.1038/nchembio.761

Orthogonal Probes def

VX-745
FS-694
SR-318

Chemical Information

Molecular Formula C24H21F2NO4
SMILEs O=C1c2ccc(Nc3ccc(F)cc3F)cc2CCc2ccc(OC[C@H](O)CO)cc21
InChI InChI=1S/C24H21F2NO4/c25-16-4-8-23(22(26)10-16)27-17-5-7-20-15(9-17)2-1-14-3-6-19(11-21(14)24(20)30)31-13-18(29)12-28/h3-11,18,27-29H,1-2,12-13H2/t18-/m1/s1
Molecular weight 425.14 Da
AlogP 0.0
HBond acceptors 5
HBond donors 3
Atoms 52

References

Publications

Cross References

canSARChEMBLBindingDBPDBPubMed

Vendors

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

Expert Reviews

by SERP
(on 18 Mar 2017 )
Cellular Use Rating
In Model Organisms
Skepinone-L is a potent, selective, and cell active p38 inhibitor. It is orally bioavailable in mice. It shows exquisite kinase selectivity, as measured by screening against broad panels at Ambit (DiscoveRx)...
by SERP
(on 2 Apr 2017 )
Cellular Use Rating
In Model Organisms
Experiments for selectivity in cells included an Ambit screen and a ProQuinase panel. Structure-activity relationships are logical and structurally based. I would like to see evidence for and against...
by SERP
(on 2 Jun 2017 )
Cellular Use Rating
In Model Organisms
Skepinone-L is a potent (5 nM) p38alpha/beta-dual inhibitor with wonderful kinome selectivity (minimal to no activity on 300+ kinases at 1 uM). It has activity in a cell-based, mechanistic...
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