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JNK-IN-8 | Covalent Inhibitor of MAPK8, MAPK9, MAPK10
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MAPK8
  • IC 50:14.7 nM
    MAPK9
    • IC 50:18.7 nM
    • IC 50:338 nM
    MAPK10
    • IC 50:1 nM
    • IC 50:486 nM
    Covalent Inhibitor
    1 nM - 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    442 kinases were tested in DiscoveRx panel, and 121 kinases were tested in radiometric assays. With ...
    Selectivity Assessment Description:
    442 kinases were tested in DiscoveRx panel, and 121 kinases were tested in radiometric assays. With ...
    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    200 kinases were assays in A375 cells using KiNativ. With in vitro data, JNK-IN-8 did not inhibit an ...
    Selectivity Assessment Description:
    200 kinases were assays in A375 cells using KiNativ. With in vitro data, JNK-IN-8 did not inhibit an ...

    Potency
    Cellular
    In Vitro

    MAPK8

    Mode of Action: Covalent Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1016/j.chembiol.2011.11.010

    MAPK9

    Mode of Action: Covalent Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1016/j.chembiol.2011.11.010

    MAPK10

    Mode of Action: Covalent Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1016/j.chembiol.2011.11.010

    Chemical Information

    Molecular Formula C29H29N7O2
    SMILEs Cc1cc(NC(=O)c2cccc(NC(=O)/C=C/CN(C)C)c2)ccc1Nc1nccc(-c2cccnc2)n1
    InChI InChI=1S/C29H29N7O2/c1-20-17-24(11-12-25(20)34-29-31-15-13-26(35-29)22-8-5-14-30-19-22)33-28(38)21-7-4-9-23(18-21)32-27(37)10-6-16-36(2)3/h4-15,17-19H,16H2,1-3H3,(H,32,37)(H,33,38)(H,31,34,35)/b10-6+
    Molecular weight 507.24 Da
    AlogP 4.89922
    HBond acceptors 9
    HBond donors 3
    Atoms 67

    References

    Publications

    Cross References

    canSARChEMBLBindingDB

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    Expert Reviews

    by SERP
    (on 20 Jun 2016 )
    Cellular Use Rating
    JNK-IN-8 is a covalent and highly selective JNK1/2/3 inhibitor with well validated activity in cells. The JNK family of kinases (also known as the stress-activated protein kinases, SAPK) play a significant...
    by SERP
    (on 21 Jun 2016 )
    Cellular Use Rating
    In Model Organisms
    This is a potent JNK1/2/3 inhibitor with some off target activity (MNK2, FMS at 200-500 nM).
    by SERP
    (on 27 May 2017 )
    Cellular Use Rating
    JNK-IN-8 is an imatinib-derived pan-JNK inhibitor (biochemical IC50 values: 4.7 nM (JNK1), 18.7 nM (JNK2), 1 nM (JNK3)). Its covalent-irreversible binding mode is reasonable validated by X-ray structures...
    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