MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2.

a first-in-class degrader of MEK1/2, MS432 (23), which potently and selectively degraded MEK1 and MEK2 in a VHL E3 ligase- and proteasome-dependent manner and suppressed ERK phosphorylation in cells.?It inhibited colorectal cancer and melanoma cell proliferation much more effectively than its negative control MS432N (24), and its effect was phenocopied by MEK1/2 knockdown.

MS432 (23)Compound 23 was highly selective for MEK1/2 in global proteomic profiling studies.?It was also bioavailable in mice and can be used for in vivo efficacy studies.?We provide two well-characterized chemical tools to the biomedical community.

T13782

C50H65F3IN7O6S

1076.06

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years