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Ruxolitinib | ATP-competitive of JAK1, JAK2
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
JAK1
  • IC 50:3.3 nM
  • IC 50:280 nM
JAK2
  • IC 50:2.8 nM
  • IC 50:280 nM
ATP-competitive
5 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - TYK2 19 nM, JAK3 428 nM

Potency Assay Off-Target:
Ruxolitinib was not active against a panel of 26 additional kinases at ~300 nM.
Selectivity Assessment Description:
Ruxolitinib was not active against a panel of 26 additional kinases at ~300 nM.
In Cell Selectivity Assessment
Potency Assay Off-Target:
In various cells, Ruxolitinib did not impact BCR-ABL or KIT signaling pathways.
Selectivity Assessment Description:
In various cells, Ruxolitinib did not impact BCR-ABL or KIT signaling pathways.

Potency
Cellular
In Vitro

JAK1

Mode of Action: ATP-competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1182/blood-2009-04-214957

JAK2

Mode of Action: ATP-competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1182/blood-2009-04-214957

In Vivo Validations

Mouse
Dose: 90 mg/kg
Route of delivery: Oral
Organ of interest (O): spleen, blood
Target engagement assay: Indirect: inhibition of protein substrate phosphorylation in white blood cells

DOI Reference: 10.1182/blood-2009-04-214957

Orthogonal Probes def

Baricitinib
FILGOTINIB

Chemical Information

Molecular Formula C17H18N6
SMILEs N#CC[C@H](C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1
InChI InChI=1S/C17H18N6/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16/h6,8-12,15H,1-5H2,(H,19,20,21)/t15-/m1/s1
Molecular weight 306.16 Da
AlogP 3.466380000000001
HBond acceptors 6
HBond donors 1
Atoms 41

References

Publications

Cross References

Vendors

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Expert Reviews

by SERP
(on 20 May 2016 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 31 May 2016 )
Cellular Use Rating
In Model Organisms
This compound inhibits JAK1 IC50 7 nM (1 mM ATP) and JAK2 IC50 9 nM (1 mM ATP) equally well. Because either JAK1 or JAK2 can be a part of any receptor pairing in any in vitro or in vivo setting, this...
by SERP
(on 24 Aug 2016 )
Cellular Use Rating
In Model Organisms
Validation for this compound is high. No significant inhibtion was observed in a panel of 26 kinases when tested at a concentration 100-fold higher than the IC50 observed for JAK1/2, though the modest...
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