Drug intelligence / Profile preview

BIX02189

Development stage
Preclinical
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

BIX02189 is a potent and selective small molecule inhibitor of Mitogen-activated protein kinase kinase 5 (MEK5), with an IC50 of approximately 1.5 nM. It exhibits high selectivity for MEK5 over other closely related kinases such as MEK1 and MEK2. By inhibiting MEK5, BIX02189 prevents the activation of the downstream Extracellular signal-regulated kinase 5 (ERK5) pathway, which is involved in cell proliferation, survival, and stress responses. In oncology research, particularly in multiple myeloma, BIX02189 has been used to demonstrate that the RBM39-MEK5 axis is essential for malignant cell survival and that its inhibition can sensitize cells to chemotherapy agents like bortezomib.

Other names
1094614-85-31265916-41-3
02

Targets

MAPK7 (ERK5)MEK5 (Mitogen-Activated Protein Kinase Kinase 5)CSF1R (Macrophage colony-stimulating factor receptor)

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