HPK1 inhibitor 1 is a highly potent, selective inhibitor of HPK1/MAP4K1 with biochemical IC50 of 0.0465 nM.
HPK1 inhibitor 1 displays >100-fold selectivity against 260 kinases in a panel of 265 kinases.
HPK1 inhibitor 1 decreased SLP-76 phosphorylation in a human pSLP-76 ELISA at an IC50 lower than 0.02 uM.
HPK1 inhibitor 1 enhanced Th1 cytokine production in T cells and fully reverted immune suppression imposed by the prostaglandin E2 (PGE2) and adenosine pathways in human T cells.
HPK1 inhibitor 1 demonstrated a synergistic effect, resulting in enhanced interferon (IFN)-γ production when combination with pembrolizumab in human PBMCs
