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.
Form:Solid
规格
规格或纯度
≥99%
英文名称
GNE-1858
生化机理
GNE-1858 是一种强效的 ATP 竞争性造血祖细胞激酶-1(HPK1)抑制剂,对野生型和活性模拟突变体 HPK1-TSEE 和 HPK1-SA 的 IC 50 s 分别为 1.9 nM、1.9 nM 和 4.5 nM。