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BIX02188-Me
- Soluble in DMSO
- MF: C26H26N4O2
- MW: 426.51
Description
BIX02188-Me is a N-methyl analogue of BIX02188 (Axon 3346) and BIX02189 (Axon 1809). BIX02188-Me is a selective dual MEK5 and ERK kinase inhibitor similar to BIX02188 and BIX02189.
The MEK5-ERK5 pathway contributes to proliferation, survival, differentiation and stress-responsive transcription. BIX02188-Me provides a related chemical tool for evaluating ERK5 pathway dependence and selectivity within MAPK signaling networks.
Key Features
- MEK5/ERK5 pathway-focused kinase inhibitor
- N-methyl analogue of BIX02188
- Useful for interrogating ERK5/BMK1 signaling
- Supports comparison with related BIX02188 and BIX02189 inhibitors
Applications
- MEK5-ERK5 pathway research
- MAPK signaling and kinase selectivity studies
- Cell proliferation and survival pathway assays
- Comparative profiling of ERK5 pathway inhibitors
More Information
| Parent CAS No. | 334951-92-7 |
|---|---|
| Chemical Name | (Z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-N-methyl-2-oxoindoline-6-carboxamide |
| extra_info | Uncertainty remains about the structure matching the name BIX 02188. Axon Medchem sells the monomethyl amide. |
| SMILES | N1C2=C(C=CC(C(NC)=O)=C2)/C(=C(/NC2=CC=CC(CN(C)C)=C2)C2=CC=CC=C2)/C1=O |
| MFCD | N.A. |
| InChi | InChI=1S/C26H26N4O2/c1-27-25(31)19-12-13-21-22(15-19)29-26(32)23(21)24(18-9-5-4-6-10-18)28-20-11-7-8-17(14-20)16-30(2)3/h4-15,28H,16H2,1-3H3,(H,27,31)(H,29,32)/b24-23- |
| InChiKey | BQNHHYZMVCQLJG-VHXPQNKSSA-N |
| CID | 135742497 |
| 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.
- E. Razumovskaya et al. Inhibition of MEK5 by BIX02188 induces apoptosis in cells expressing the oncogenic mutant FLT3-ITD. Biochem. Biophys. Res. Commun. 2011, 412, 307-312.
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