Chemical Probes logo
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
Vendors
Download

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

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

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