compound introduction
GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC 50 s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively. In Vitro Hematopoietic progenitor kinase-1 (HPK1), a serine/threonine Ste20-related protein kinase whose expression is restricted to the hematopoietic compartment (e.g., T cells, B cells, and dendritic cells), is one such kinase. HPK1 is a negative-feedback regulator of T cell receptor signaling, which dampens T cell proliferation and effector function. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
