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ERK5-IN-1 is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 μM in HEK293 cells. The pAP1-luciferase reporter and pRL-CMV-Renilla plasmids were co-transfected with plasmids encoding for ERK5 and constitutively active MEK5 (MEK5DD) in HEK293 cells. Cells were treated with the indicated amounts of compound 26 (XMD17-109) for 24 h, and lysates were subjected to the dual-luciferase assay. Compound 26 completely inhibited the ERK5-mediated AP1 transcriptional activity at 30 μM and had an EC50 of 4.2 ± 0.7 μM.
| Molecular Weight | 638.8 |
| Formula | C36H46N8O3 |
| CAS Number | 1435488-37-1 |
| Solubility (25°C) | DMSO ≥ 70 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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