Preferred Label : Hpk1 Inhibitor GRC 54276;
NCIt definition : An orally bioavailable small molecule inhibitor of the serine/threonine enzyme hematopoietic
progenitor kinase 1 (Hpk1; Hpk-1; mitogen-activated protein kinase kinase kinase kinase
1; MAP4K1; MEKKK1), with potential immunostimulating and antineoplastic activities.
Upon oral administration, Hpk1 inhibitor GRC 54276 targets, binds to and inhibits
the activity of Hpk1. This inhibits Hpk1-mediated signaling pathways and prevents
Hpk1-mediated immunosuppression by preventing the inhibition of T cell receptors (TCR)
signaling and effector T-cells, disrupting abnormal cytokine expression, and abrogating
the immunosuppressive tumor microenvironment (TME). This may activate a cytotoxic
T-lymphocyte (CTL)-mediated immune response against tumor cells. Hpk1, expressed in
hematopoietic cells, is a negative regulator of TCR signaling and T- and B-cell activation.;
Molecule name : GRC-54276; GRC 54276;
NCI Metathesaurus CUI : CL1915093;
Origin ID : C200829;
UMLS CUI : C5854608;
Semantic type(s)
- concept_is_in_subset
- has_target
