PROTAC MEK1 Degrader-1_product_DataBase

Bioactivity	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[1].
Invitro	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[1]。PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 12 h) 显著抑制 IL6 等细胞因子的分泌[1]。PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 0-72 h) 对 A375 细胞具有抗增殖活性[1]。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[1]。 Cell Proliferation Assay[1] Cell Line:
Name	PROTAC MEK1 Degrader-1
CAS	2671004-41-2
Formula	C53H66FIN8O11S2
Molar Mass	1201.17
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Vollmer S, et al. Design, Synthesis, and Biological Evaluation of MEK PROTACs. J Med Chem. 2020 Jan 9;63(1):157-162.

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