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Baricitinib | Inhibitor of JAK1, JAK2
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 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 50:5.9 nM
    JAK2
    • IC 50:5.7 nM
    • IC 50:44 nM
    • IC 50:128 nM
    • IC 50:20 nM
    • IC 50:40 nM
    Inhibitor
    up to 100 nM

    Selectivity

    In Vitro Selectivity Assessment

    Potency: IC50 - Tyk2 53 nM, JAK3 560 nM, AAK1 17.2 nM, BIKE 39.8 nM, GAK134.4 nM, MPSK1 68.5 nM

    Potency Assay Off-Target:
    TR-FRET, ITC
    Selectivity Assessment Description:
    JAK3 IC50 ~ 560 nM, ~10-fold selectivity against Tyk2 (IC50 = 53 nM), c-Met (IC50 > 10,000 nM) ...

    Potency
    Cellular
    In Vitro

    JAK1

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.4049/jimmunol.0902819

    JAK2

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.4049/jimmunol.0902819

    In Vivo Validations

    Mouse, Rat
    Dose: 1, 3, 10 mg/Kg
    Route of delivery: Oral

    DOI Reference: 10.4049/jimmunol.0902819

    Negative Control Compounds

    INCB027753
    INCB029843

    Orthogonal Probes def

    Ruxolitinib
    Filgotinib

    Chemical Information

    Molecular Formula C16H17N7O2S
    SMILEs CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1
    InChI InChI=1S/C16H17N7O2S/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20)
    Molecular weight 371.12 Da
    AlogP 1.09568
    HBond acceptors 9
    HBond donors 1
    Atoms 43

    References

    Publications

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    Expert Reviews

    by SERP
    (on 15 Apr 2025 )
    Cellular Use Rating
    In Model Organisms
    Baricitinib (alternatively named INCB28050, LY3009104) is an FDA-approved drug and a potent inhibitor of JAK1/2 with a decent in vivo profile. Baricitinib, however, is insufficiently profiled for use as...
    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