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BIX 02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM. BIX 02189 inhibited catalytic function of purified, MEK5 enzyme. The MEK5 inhibitors blocked phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. BIX 02189 also inhibited transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade, in a cellular trans-reporter assay system.
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Source | Sci Rep (2018). Figure 3. BIX 02189 |
| Method | cell proliferation assay | |
| Cell Lines | colorectal cancer cells | |
| Concentrations | 100 nM to 30 μM | |
| Incubation Time | 24 or 48 h | |
| Results | The data suggested that doses of BIX02189 that completely inhibited ERK5 signaling had no effect on cell proliferation |
| Molecular Weight | 440.54 |
| Formula | C27H28N4O2 |
| CAS Number | 1094614-85-3 |
| Solubility (25°C) | DMSO 48 mg/mL Ethanol 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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