HPK1-IN-3 是一种有效的选择性 ATP 竞争性造血祖细胞激酶 1 (HPK1; MAP4K1) 抑制剂，IC50 为 0.25 nM。HPK1-IN-3 具有 IL-2 细胞效力，在人外周血单核细胞 (PBMC) 中的 EC50 为 108 nM。
货号:ajcx33872
CAS:N/A
分子式:C23H22F4N6O2
分子量：490.45
溶解度:DMSO : 83.33 mg/mL (169.91 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM. HPK1-IN-3 has IL-2 cellular potency with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs)[1].

HPK1-IN-3 (compound 27; 0.25-4 μM; 24-h) treatment shows a statistically significant elevation of proinflammatory cytokines IL-6 and TNF-α was observed in a concentration-dependent manner in human monocyte-derived dendritic cells[1].

[1]. Brandon A Vara, et al. Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds. ACS Med Chem Lett. 2021 Mar 19;12(4):653-661.