PROTACHPK1 Degrader-5 is a potent, orally active HPK1 PROTAC degrader with a DC50 of 5.0 nM and a Dmax of at least 99%. It significantly inhibits HPK1 by degrading it, reducing SLP76 phosphorylation, and enhancing ERK pathway activation, which in turn stimulates the release of IL-2 and IFN-gamma. This compound effectively counteracts immune suppression induced by PGE2, NECA, or TGF-beta. Alone, PROTACHPK1 Degrader-5 is capable of suppressing tumor growth in MC38 syngeneic mouse models. It is used in research for immunotherapy applications in cancers such as colorectal cancer.
Target-Kategorie:
IFNAR|||MAPK|||PROTACs|||Interleukin|||ERK
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