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BIX-02188 | BIX-02188 : Inhibitor of MAP2K5
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
MAP2K5
  • IC50:4.3 nM
Inhibitor
3-10 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - MEK5 810 nM, CSF1R 280 nM, KIT 550 nM, LCK 390 nM

Potency Assay Off-Target:
BIX-02188 was 100-fold selective for MAP2K5 against 87 kinases.
In Cell Selectivity Assessment
Potency Assay Off-Target:
In HeLa cells, BIX-02188 did not inhibit p38 or JNK signaling pathways

Potency
Cellular
In Vitro

MAP2K5

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Chemical Information

Molecular Formula C25H24N4O2
SMILEs CN(C)Cc1cccc(N/C(=C2\C(=O)Nc3cc(C(N)=O)ccc32)c2ccccc2)c1
InChI InChI=1S/C25H24N4O2/c1-29(2)15-16-7-6-10-19(13-16)27-23(17-8-4-3-5-9-17)22-20-12-11-18(24(26)30)14-21(20)28-25(22)31/h3-14,27H,15H2,1-2H3,(H2,26,30)(H,28,31)/b23-22-
Molecular weight 412.19 Da
AlogP 3.779600000000002
HBond acceptors 6
HBond donors 4
Atoms 55

References

Publications

    Cross References

    canSARChEMBLBindingDB

    Vendors

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    Expert Reviews

    by SERP
    (on 11 Jun 2016 )
    Cellular Use Rating
    Assays used to discover these compounds and the cell-based assay all use firefly luciferase. While the in vitro data shows convincing activity - (nM) potency - for MEK5 inhibition with selectivity against...
    by SERP
    (on 3 Jan 2017 )
    Cellular Use Rating
    In Model Organisms
    There is limited literature surrounding BIX-02188. It is reported to be a selective inhibitor of MEK5 (Mitogen-activated protein kinases kinase, MAP2K). The MEK class of enzymes is comprised of seven...
    by SERP
    (on 20 Jan 2017 )
    Cellular Use Rating
    This report identifies two compounds, BIX02188 and BIX02189, as potent inhibitors of the kinase MEK5, and thus of the MEK/ERK pathway. The approved symbol for MEK5 is MAP2K5, so one may see this in the...
    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