PROTAC HPK1 Degrader-3

MedChem Express

PROTAC PD-L1 degrader-2

9

Research Use Only

C43H42N8O5

750.84

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-kappaB 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%. PROTAC HPK1 Degrader-3 is composed of E3 ligase ligand Thalidomide (HY-14658; blue part), PROTAC linker tert-Butyl 3-oxoazetidine-1-carboxylate (HY-40146; black part), and target protein ligand HPK1-IN-51 (HY-162842; red part); the activity control of the target protein ligand can be HPK1 ligand 1 (HY-162841)[1].

CN(C(C(C=CC(C1=CNC2=C1N=C(C=N2)C3=CC=C(C=C3)C4CCN(CC4)C5CN(C6=CC=C7C(C(N(C7=O)C8C(NC(CC8)=O)=O)=O)=C6)C5)=C9)=C9C)=O)C

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