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| Molecular Weight (MW) | 440.54 |
|---|---|
| Formula | C27H28N4O2 |
| CAS No. | 1094614-85-3 |
| Synonyms |
N/A
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| Solubility (25°C) | DMSO 88 mg/mL |
| Water <1 mg/mL | |
| Ethanol 88 mg/mL | |
| Stability | 2 years-20°CPowder |
| 2 weeks4°Cin DMSO | |
| 6 months-80°Cin DMSO |
BIX 02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM. [1] It 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. The compounds also inhibited transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade, in a cellular trans-reporter assay system. [2]
[1] Biochemical and Biophysical Research Communications 2008;377：120–125
[2] JOURNAL OF BIOLOGICAL CHEMISTRY August 28, 2009;284：23564–23573
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Effects of BIX02189 on cadmium-induced apoptosis in HK-2 cells. (A) PARP cleavage. Cells were preincubated with 0.1% DMSO or 20 lM BIX02189 for 1 h, then incubated with 0, 20, or 50 lM CdCl2 for 16 h. Cell lysates were subjected to Western immunoblotting using antibodies against PARP and actin. Full-length and cleaved forms of PARP were detected at 116- and 89-kDa, respectively. Results are representative of at least four experiments. (B) Cytoplasmic nucleosomes. Cells were preincubated with 0.1% DMSO or 20 lM BIX02189 for 1 h, then incubated with or without 20 lM CdCl2 for 16 h. The cytoplasmic fraction was used for a nucleosomes ELISA. Each value (mean ± S.E.M., n = 5–7) represents the fold increase with respect to untreated control (without BIX02189 or CdCl2). Results are representative of four experiments. |
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Inhibition of ERK5 suppresses Nrf2 nuclear translocation in mouse aorta in vivo. Nrf2 nuclear translocation in mouse aortic endothelium was analyzed by en face immunofluorescence staining assay using anti-Nrf2 antibody (red). Mice were treated with either 10 mg/kg of BIX02189 (in 25% DMSO) or vehicle control (same volume of 25% DMSO) by ntraperitoneal injection. Endothelium of thoracic aorta was stained with anti-vascular endothelial-cadherin (VE-cadherin) antibody for endothelial cell-cell junction staining (green), Topro3 for nuclear staining (blue), and anti-Nrf2 antibody (red) and photographed under a confocal microscope.. |
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Inhibition of ERK5 suppresses laminar flow-mediated Nrf2-dependent gene expression. B, HUVECs were exposed to atheroprotective flow for 16–24 h in the presence of either DMSO or BIX02189 (10uM). Protein expression of HO-1, NQO1, eNOS, pERK5, ERK5, and tubulin was determined by immunoblotting with specific antibodies. Data are representative from three independent experiments. |
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Expression of iNOS, Fra-1, Fra-2, JunB, JunD, and FosB in PMN. (A) PMN were treated with or without SB203580 (40 μM), BIX02189 (30 μM), or SP600125 (40 μM) for 1 h before addition of NDMA (0.74 μg/μl). The cytoplasmic and nuclear fractions obtained from the cells were used to detect iNOS, Fra-1, Fra-2, JunB, JunD, and FosB protein levels by Western blot. The results shown are representative of five independent experiments. |
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Effects of BIX02189 on cadmium-induced accumulation of phosphorylated ERK5, phosphorylated ERK1/2, phosphorylated CREB, and c-Fos proteins in HK-2 cells. Cells were preincubated with 0.1% DMSO or 5, 10, 20, or 50 uM BIX02189 for 1 h, then incubated with or without 50 uM CdCl2 for 2 (top four panels) or 4 h (bottom four panels). Cell lysates were subjected to Western immunoblotting using antibodies against phospho-ERK5, ERK5, phospho-ERK1/2, ERK1/2, phospho-CREB, CREB, c-Fos, and actin. Results are representative of at least three experiments. |
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T47D cells were pretreated 30 minutes BIX 02189(0,10,20,30,50 μM) and then co-incubated with Heregulin + BIX 02189 for 15 minutes. |
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BIX 02189 Chemical Structure
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