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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

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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

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Expert Reviews

by SERP
(on 20 May 2016)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public 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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