Bioactivity | PROTAC PD-L1 degrader-3 (Compound B3) is an orally active PROTAC degrader for PD-L1 with a DC50 of 0.5 μM. PROTAC PD-L1 degrader-3 exhibits inhibitory activity against PD-1/PD-L1 interaction with an IC50 of 22.8 nM. PROTAC PD-L1 degrader-3 upregulates the expressions of Atg9b, Lamp1 and Mitf, and activates the autophagy lysosome system. PROTAC PD-L1 degrader-3 exhibits antitumor efficacy in CT26 mouse model. (Pink: Ligand for target protein (HY-159894); Black: Linker (HY-W015088); Blue: Ligand for E3 ligase (HY-169365))[1] |
Formula | C45H48N8O5 |
Molar Mass | 780.91 |
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]. Wang K, et al., Discovery of small molecules for autophagy-lysosome degradation of immune checkpoint proteins. Eur J Med Chem. 2024 Dec 15;280:116958. |