产品
编 号：F754505
分子式：C53H66FIN8O11S2
分子量：1201.17
分子式：C53H66FIN8O11S2
分子量：1201.17
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规格
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CAS No: 2671004-41-2
产品详情
生物活性：
PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells.
体外研究：
PROTAC MEK1 Degrader-1 (Compound 3) (10 μM-100 pM; 12 h) 在 1 μM 和 10 μM 两个最高浓度下发生降解，而较低浓度则导致 MEK1 和 ERK1/2 表达增加。PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 12 h) 显著抑制 IL6 等细胞因子的分泌。PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 0-72 h) 对 A375 细胞具有抗增殖活性。PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 0-20 h) 可在 5 h 后显著降解 MEK 和 ERK1/2，8 h 后完全抑制。
PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells.
体外研究：
PROTAC MEK1 Degrader-1 (Compound 3) (10 μM-100 pM; 12 h) 在 1 μM 和 10 μM 两个最高浓度下发生降解，而较低浓度则导致 MEK1 和 ERK1/2 表达增加。PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 12 h) 显著抑制 IL6 等细胞因子的分泌。PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 0-72 h) 对 A375 细胞具有抗增殖活性。PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 0-20 h) 可在 5 h 后显著降解 MEK 和 ERK1/2，8 h 后完全抑制。
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