ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC 50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy , and can be used to study NSCLC (Non-small cell lung cancer) 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. ULK1-IN-2 (0-8 μM, 24 h) blocks autophagy via inhibiting ULK1 in A549 cells. ULK1-IN-2 (0-8 μM, 24 h) induces apoptosis via the mitochondrial pathways in A549 cells in dose department manner. ULK1-IN-2 (0-8 μM, 24 h) inhibits ULK1 and p-ULK1 ser317 expression in a concentration-dependent manner, remarkably decreases Bcl-2 expression, increases Bax and the active form of Caspase-3 expression.. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay Cell Line: Human cancer cell lines A549, U937, HL60, MDA-MB-468 and MCF-7Concentration: 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 IC 50 values of 1.94, 12.92, 10.89, 16.83, and 19.60 μM, respectively. Cell Autophagy Assay Cell Line: A549 cellsConcentration: 0, 2, 4, 8 μM Incubation Time: 24 h Result: Blocked autophagy of A549 cells via inhibiting ULK. Western Blot Analysis Cell Line: A549 cellsConcentration: 0, 2, 4, 8 μM Incubation Time: 24 h Result: Inhibited expression of ULK1 and p-ULK1 ser317 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. Form:Solid IC50& Target:ULK1
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ULK1-IN-2
CAS number：2497409-01-3 molecular formula：C19H16BrFN4O6
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2497409-01-3 | molecular formula | C19H16BrFN4O6 |
| molecular weight | 495.26 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
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