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FM-381 | Covalent Inhibitor of JAK3
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 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
JAK3
  • IC50(app):0.154 nM
  • EC50:100 nM
Covalent Inhibitor
100 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50(app) - JAK1: 52 nM, JAK2: 346 nM, TYK2: 459 nM, BTK >5 uM, ITK: 1.8 uM, EGFR >5 uM

Potency Assay Off-Target:
In addition to assays assessing acivity against closely related kinases and those with a Cys compara ...
Selectivity Assessment Description:
FM-381 was largely inactive against a panel of bromodomain proteins. The most potent activity was ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
In human CD4+ T cells, FM-381 did not inhibit IL-6-stimulated STAT3 phosphorylation at 1 uM.

Potency
Cellular
In Vitro

JAK3

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.chembiol.2016.10.008

Negative Control Compounds

canSAR3595486
Notes: The inactive control FM-479 has no activity on JAK3 or other kinases when used at similar concentration.

Orthogonal Probes def

TOFACITINIB
JAK3i
NIBR3049

Chemical Information

Molecular Formula C24H24N6O2
SMILEs CN(C)C(=O)/C(C#N)=C/c1ccc(-c2nc3cnc4[nH]ccc4c3n2C2CCCCC2)o1
InChI InChI=1S/C24H24N6O2/c1-29(2)24(31)15(13-25)12-17-8-9-20(32-17)23-28-19-14-27-22-18(10-11-26-22)21(19)30(23)16-6-4-3-5-7-16/h8-12,14,16H,3-7H2,1-2H3,(H,26,27)/b15-12+
Molecular weight 428.20 Da
AlogP 4.6729800000000035
HBond acceptors 8
HBond donors 1
Atoms 56

Vendors

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Expert Reviews

by SERP
(on 27 Apr 2017 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 5 May 2017 )
Cellular Use Rating
This is a highly selective probe for JAK3 compared with close family members (and the wider Kinome) with parallel cellular selectivity disclosed.
by SERP
(on 1 Jun 2017 )
Cellular Use Rating
( The reviewer did not leave any comments )
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