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