| Bioactivity | 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[1]. |
| Target | Ki: 107 nM (PCSK9) |
| Invitro | 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]. Western Blot Analysis[1] Cell Line: |
| Name | PCSK9 degrader 1 |
| Formula | C53H69FN8O13S |
| Molar Mass | 1077.22 |
| 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]. 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. |