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BIX 02189
- Soluble in DMSO
- MF: C27H28N4O2
- MW: 440.54
Description
BIX02189 is a selective dual MEK5 and ERK5/BMK1 inhibitor with IC50 values of 1.5, 59, 580 and >6200 nM for MEK5, ERK5, TGFbR1 and other closely related kinases respectively. BIX02189 is a close analogue of BIX02188-Me (Axon 1808) and BIX02188 (Axon 3346).
MEK5-ERK5 signaling regulates transcriptional responses linked to proliferation, vascular biology and stress adaptation. BIX 02189 is used to dissect ERK5 pathway signaling and to distinguish MEK5/ERK5 biology from other MAPK cascades.
Key Features
- Dual MEK5 and ERK5/BMK1 inhibitor
- Reported IC50: 1.5 nM for MEK5 and 59 nM for ERK5
- Shows weaker activity against TGFβR1 and limited activity against related kinases
- Useful probe for ERK5 pathway inhibition
Applications
- MEK5-ERK5/BMK1 signaling studies
- MAPK pathway selectivity profiling
- Cell proliferation and transcriptional response assays
- Kinase inhibitor comparison and pathway validation
More Information
| Parent CAS No. | 1094614-85-3 |
|---|---|
| Chemical Name | ((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide |
| SMILES | N1C2=C(C=CC(C(N(C)C)=O)=C2)/C(=C(/NC2=CC=CC(CN(C)C)=C2)C2=CC=CC=C2)/C1=O |
| MFCD | N.A. |
| InChi | InChI=1S/C27H28N4O2/c1-30(2)17-18-9-8-12-21(15-18)28-25(19-10-6-5-7-11-19)24-22-14-13-20(27(33)31(3)4)16-23(22)29-26(24)32/h5-16,28H,17H2,1-4H3,(H,29,32)/b25-24- |
| InChiKey | HOMJAAIVTDVQJA-IZHYLOQSSA-N |
| CID | 135659062 |
| Short Description | MEK5/ERK5 inhibitor |
References
- RJ Tatake et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem. Biophys. Res. Comm. 2008, 377(1), 120–125.
- Y Obara and N Nakahata. The signaling pathway leading to extracellular signal-regulated kinase 5 (ERK5) activation via G-proteins and ERK5-dependent neurotrophic effects. Mol. Pharmacol. 2010, 77(1), 10-16.
- BA Drew, ME Burowa , BS Beckman. MEK5/ERK5 pathway: The first fifteen years. Biochimica et Biophysica Acta (BBA) - Reviews on Cancer 2012, 1825 (1), 37-48.
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