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PCSK9 degrader 1

Catalog No.GC70635

PCSK9 degrader 1 (composé 16) est une petite molécule Ligand de la proprotéine convertase subtilis Protease - like / Kexin type 9 (pcsk9) présentant une affinité élevée pour la pcsk9 avec un ki de 107 nm.

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PCSK9 degrader 1 Chemical Structure

Taille Prix Stock Qté
1 mg
630,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents
PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor.

PCSK9 degrader 1 (Compound 16; 1.25-20 μM; 24 hours; HEK293 cells) treatment shows a clear concentration-dependent degradation of both the pro and mature form of PCSK9 yielding a half-maximal degradation concentration of 4.8 and 3.4 μM, as well as a maximum percentage of degradation at 20 μM of 58% and 61%, respectively[1].

References:
[1]. Petrilli WL, et al. From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9. Cell Chem Biol. 2019 Oct 22. pii: S2451-9456(19)30322-8.

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