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PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1/2 phosphorylation. With a pIC50 value of 7.0, it exhibits antiproliferative activity against A375 cells [1].
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5 mg | Inquiry | Backorder | |
50 mg | Inquiry | Backorder |
Description | PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1/2 phosphorylation. With a pIC50 value of 7.0, it exhibits antiproliferative activity against A375 cells [1]. |
In vitro | PROTAC MEK1 Degrader-1 (Compound 3) induces MEK1 degradation at concentrations of 1 μM and 10 μM over 12 hours, while lower concentrations increase MEK1 and ERK1/2 expression [1]. At 10 μM, it significantly inhibits IL6 secretion over 12 hours and shows anti-proliferative activity against A375 cells from 0 to 72 hours [1]. Significant MEK and ERK1/2 degradation occurs at 5 hours post-treatment with 10 μM, with complete inhibition at 8 hours [1]. |
Molecular Weight | 1201.17 |
Formula | C53H66FIN8O11S2 |
Cas No. | 2671004-41-2 |
Storage | Shipping with blue ice. |
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