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JNK2_3 COV56d | JNK2/3 COV56d : Covalent Inhibitor of MAPK9, MAPK10
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MAPK9
  • IC50:25 nM
  • Kd:15 nM
  • IC50:830 nM
  • EC50:883 nM
MAPK10
  • IC50:40 nM
  • Kd:5 nM
  • IC50:1909 nM
    Covalent Inhibitor
    up to 5 uM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Selective 11x over JNK1 as confirmed by NanoBRET
    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Kinome screening was carried out in a representative panel consisting of 97 kinases (scanEDGE─KINOME ...

    Potency
    Cellular
    In Vitro

    MAPK9

    Mode of Action: Covalent Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.5c00884

    MAPK10

    Mode of Action: Covalent Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.5c00884

    Orthogonal Probes def

    CTx-0294885

    Chemical Information

    Molecular Formula C30H24N6O3
    SMILEs C=CC(=O)Nc1cccc(C(=O)Nc2cccc(-n3cc(NC(=O)Nc4cccc5ccccc45)cn3)c2)c1
    InChI InChI=1S/C30H24N6O3/c1-2-28(37)32-22-11-5-10-21(16-22)29(38)33-23-12-7-13-25(17-23)36-19-24(18-31-36)34-30(39)35-27-15-6-9-20-8-3-4-14-26(20)27/h2-19H,1H2,(H,32,37)(H,33,38)(H2,34,35,39)
    Molecular weight 516.19 Da
    AlogP 6.046300000000004
    HBond acceptors 9
    HBond donors 4
    Atoms 63

    References

    Publications

    Cross References

    Expert Reviews

    by SERP
    (on 17 Aug 2025 )
    Cellular Use Rating
    In cell based assays, JNK2_3 Cov56d should provide selective inhibition of JNK2 verse JNK1 when used at concentrations of 1-5 uM. However, the potency of the probe against JNK3 in cells in not known and...
    by SERP
    (on 21 Aug 2025 )
    Cellular Use Rating
    56d is likely a useful compound to probe MAPK9 and 10 (JNK2 and 3) function. It has an ATP-competitive, covalent mechanism of action with impressive kinact/KI. This compound shows very limited in vitro...
    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