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].
Molecular Weight:
750.84
Formula:
C43H42N8O5
Target:
MAP4K,PROTACs
Application Notes:
MCE Product type: Reference compound
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