ULK抑制剂;ULK Inhibitors;产品介绍:SBI-0206965 是一种高度选择性自吞噬激酶ULK1抑制剂,IC50为108 nM,选择性比作用于ULK2高7倍。SBI-0206965 可抑制人胶质母细胞瘤和肺癌细胞中的自噬而增强凋亡。;InformationSBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.TargetsULK1 (Cell-free assay); ULK2 (Cell-free assay) 108 nM; 711 nMIn vitroIn HEK293T transfected with WT or KI Myc-tagged ULK1 and WT Vps34, SBI-0206965 inhibits Ser249 phosphorylation of overexpressed Vps34 and Beclin1 Ser15 phosphorylation. SBI-0206965 suppresses autophagy induced by mTOR inhibition in A549 cells, and prevents ULK1-dependent cell survival in WT MEFs. In addition, SBI-0206965 also synergizes with mTOR inhibition to induce cancer cell death.