PCSK9 degrader 1

PCSK9 degrader 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) degrader. PCSK9 degrader 1 does not affect PCSK9 function[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> Ser/Thr Protease

Research Areas >> Cancer

Biphenyl acid PCSK9 degrader 1 (compound 9) binds to and thermally stabilizes PCSK9 in a complex environment such as Huh7 lysate[1]. PCSK9 degrader 1 (compound 9), with high affinity for recombinant PCSK9 and target engagement in cell lysate, could be used as a recruiting element to promote the selective degradation of PCSK9[1].

[1]. Whitney L Petrilli, et al. From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9. Cell Chem Biol. 2020 Jan 16;27(1):32-40.e3.