Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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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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) causes degradation at the two highest concentrations of 1 μM and 10 μM over a 12-hour period, while lower concentrations result in increased expression of MEK1 and ERK1/2 [1]. At a concentration of 10 μM, it significantly inhibits the secretion of cytokines such as IL6 over 12 hours [1]. The compound demonstrates anti-proliferative activity against A375 cells from 0 to 72 hours at a concentration of 10 μM [1]. Furthermore, 5 hours post-treatment with 10 μM, there is a significant degradation of MEK and ERK1/2, with complete inhibition observed at 8 hours [1]. |
Molecular Weight | 1201.17 |
Formula | C53H66FIN8O11S2 |
CAS No. | 2671004-41-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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PROTAC MEK1 Degrader-1 2671004-41-2 PROTAC PROTACs inhibitor inhibit