GNE-1858 是高效的 ATP 竞争性造血祖细胞激酶-1抑制剂,能够抑制野生型(IC50:1.9 nM)、活性模拟突变株 HPK1-TSEE (IC50:1.9 nM)、 HPK1-SA (IC50:4.5 nM)的活性。
产品描述
GNE-1858 is an ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor (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).
体外活性
HPK1 is a negative-feedback regulator of T cell receptor signaling, which dampens T cell proliferation and effector function.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.?
Cas No.
2680616-96-8
分子式
C21H26F2N8
分子量
428.48
储存和溶解度
DMSO:15 mg/mL (35.01 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years