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BIX02188 is a selective inhibitor of mitogen-activated protein kinases kinase 5 (MEK5). BIX02188 significantly blocks MEK5 catalytic activity with IC50 of 4.3 nM and inhibits ERK5 catalytic activity with IC50 of 0.81 μM. BIX02188 inhibits transcriptional activation of MEF2C through the MEK5/ERK5 signaling cascade in active MEK5/ERK5/MEF2C-driven luciferase expression system in HeLa and HEK293 cells. BIX02188 also inhibits phosphorylation of BMK1 in bovine lung microvascular endothelial cells (BLMECs) by blocking the MEK5 signal pathway, in a dose-dependent manner with IC50 of 0.8 μM.
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Source | Biochem Biophys Res Commun (2014). Figure 4. BIX02188 |
| Method | ERK5 inhibition by BIX02188 | |
| Cell Lines | NP cells | |
| Concentrations | 5 μM | |
| Incubation Time | 48 h | |
| Results | After treatment of NP cells by BIX02188 (5 lM) for 48 h, the mRNA expression of type II collagen and aggrecan was significant decreased (P < 0.05) |
| Molecular Weight | 412.48 |
| Formula | C25H24N4O2 |
| CAS Number | 1094614-84-2 |
| Solubility (25°C) | DMSO 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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