| In Vitro |
ULK1-IN-2 (compound 3s) (10 μM, 24 h) shows strong anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7[1]. ULK1-IN-2 (0-8 μM, 24 h) blocks autophagy via inhibiting ULK1 in A549 cells[1]. ULK1-IN-2 (0-8 μM, 24 h) induces apoptosis via the mitochondrial pathways in A549 cells in dose department manner[1]. ULK1-IN-2 (0-8 μM, 24 h) inhibits ULK1 and p-ULK1ser317 expression in a concentration-dependent manner, remarkably decreases Bcl-2 expression, increases Bax and the active form of Caspase-3 expression.[1]. Cell Proliferation Assay Cell Line: Human cancer cell lines A549, U937, HL60, MDA-MB-468 and MCF-7[1] Concentration: 10 μM Incubation Time: 24 h Result: Significantly improved anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7, with kinase inhibitory activity of 99.15% and IC50 values of 1.94, 12.92, 10.89, 16.83, and 19.60 μM, respectively. Cell Autophagy Assay Cell Line: A549 cells[1] Concentration: 0, 2, 4, 8 μM Incubation Time: 24 h Result: Blocked autophagy of A549 cells via inhibiting ULK. Western Blot Analysis Cell Line: A549 cells[1] Concentration: 0, 2, 4, 8 μM Incubation Time: 24 h Result: Inhibited expression of ULK1 and p-ULK1ser317 in a concentration-dependent manner. Increased the autophagy substrate P62, reduced LC3-I conversion to LC3-II, and decreased the levels of Beclin1. Remarkably decreased Bcl-2 expression, increased Bax and the active form of Caspase-3 expression.
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