GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s 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.
体外研究
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.
分子量
428.48
CAS号
2680616-96-8
运输条件
Room temperature in continental US; may vary elsewhere.