MAP4K Degrader

PROTAC HPK1 Degrader-1 (Compound B1) is a potent HPK1 degrader with DC₅₀ value of 1.8 nM. PROTAC HPK1 Degrader-1 inhibits phosphorylation of the SLP76 protein with IC₅₀ value of 496.1 nM. PROTAC HPK1 Degrader-1 is a bona fide HPK1-PROTAC degrader, which provided a potential tool for further HPK1 investigation in TCR signaling.

DD205-291 is an orally active PROTAC HPK1 degrader, with a DC₅₀ value of 5.3 nM. DD205-291 inhibits SLP-76 phosphorylation and induces IL-2 and IFN-γ expression (Pink: HPK1 protein ligand HY-168283; E3+linker: HY-168284; Blue: E3: HY-W115490; Black: linker: HY-W210252).

PROTAC HPK1 Degrader-2 (compound 3) is a PROTAC degrader of HPK1, with the DC₅₀ of 23 nM in human PBMC. PROTAC HPK1 Degrader-2 plays an important role in cancer research.

PROTAC HPK1 Degrader-4 (compound E3) is a selective and orally active PROTAC HPK1 degrader with a DC₅₀ of 3.16 nM. PROTAC HPK1 Degrader-4 demonstrates >1000-fold selectivity over GLK. PROTAC HPK1 Degrader-4 promotes immune activation. PROTAC HPK1 Degrader-4 can be used for the study of colon cancer and lymphoma (Pink: ligand for target protein (HY-174355); Blue: ligand for E3 ligase CRBN (HY-45808); Black: Linker (HY-174356); Target protein ligand-linker Conjugate (HY-174357)).

PROTAC HPK1 Degrader-6 (314) is a highly efficient and effective PROTAC degrader targeting HPK1 (IC₅₀ ＜ 50 nM). PROTAC HPK1 Degrader-6 can be used for the study of leukemia. Red: HPK1 ligand (HY-179196); Blue: E3 ligase CRBN ligand (HY-179197).