Biological Activity
Selective MEK5 and ERK5 inhibitor (IC50 values are 1.5 and 59 nM respectively). Inhibits sorbitol-induced ERK5 phosphorylation in HeLa cells. Selective for MEK5 and ERK5 over MEK1/2, ERK1/2 and a panel of 87 kinases. Induces apoptosis in acute myeloid leukemia tumor cells.
Compound Libraries
BIX 02189 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 440.54 |
| Formula | C27H28N4O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1265916-41-3 |
| PubChem ID | 46931012 |
| InChI Key | HOMJAAIVTDVQJA-IZHYLOQSSA-N |
| Smiles | O=C2NC1=CC(C(N(C)C)=O)=CC=C1/C2=C(C4=CC=CC=C4)/NC3=CC(CN(C)C)=CC=C3 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 44.05 | 100 | |
| DMSO | 44.05 | 100 | |
| ethanol | 44.05 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 440.54. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.27 mL | 11.35 mL | 22.7 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.54 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.27 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Tatake et al (2008) Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem.Biophys.Res.Comm. 377 120 PMID: 18834865
Lopez-Royuela et al (2014) Extracellular-signal-regulated kinase 5 modulates the antioxidant response by transcriptionally controlling Sirtuin 1 expression in leukemic cells. Int.J.Biochem.Cell Biol. 53 253 PMID: 24880091
Kimura et al (2010) Targeted deletion of the extracellular signal-regulated protein kinase 5 attenuates hypertrophic response and promotes pressure overload-induced apoptosis in the heart. Circ.Res. 106 961 PMID: 20075332
Keywords: BIX 02189, supplier, BIX02189, selective, MEK5, ERK5, inhibitors, inhibits, MAPK, signaling, MEK, ERK, MEK, Tocris Bioscience
