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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 |
| Related ERK Products |
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SCH772984 is a novel and selective inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively. |
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FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 And ERK2, respectively. |
| GDC-0994
Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor with IC50 of 6.1 nM and 3.1 nM against ERK1 and ERK2, respectively. |
| Astragaloside IV
Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. |
| Corynoxeine
Corynoxeine, isolated from the hook of Uncaria Rhynchophylla, is a potent ERK1/ERK 2 inhibitor in the proliferation of PDGF-BB induced vascular smooth muscle cells (VSMCs). |
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