PROTAC HPK1 Degrader-3

PROTAC HPK1 Degrader-3 (compound C3) is an orally effective PROTAC targeting HPK1 (DC₅₀=21.26 nM). HPK1 is a negative regulator of T cell receptors, which can lead to T cell dysfunction after abnormal activation. PROTAC HPK1 Degrader-3 can inhibit SLP76 and NF-κB signaling pathways and inhibit MAPK signal transduction, and has anticancer activity and immune activation. PROTAC HPK1 Degrader-3 has a certain oral bioavailability and can be combined with PD-L1 antibody therapy to achieve a tumor growth inhibition rate of 65.58%^{[1].
(Pink: HPK1 ligand (HY-162842); Blue: Cereblon ligand (HY-14658); Black: linker (HY-40146)).}

• Data Sheet (266 KB)