LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 ( ULK1 ) activator ( EC 50 =18.94 nM) for the research of triple negative breast cancer (TNBC) In Vitro LYN-1604 is a potential ULK1 agonist (enzymatic activity=195.7% at 100 nM and IC 50 =1.66 μM against MDA-MB-231 cells). LYN-1604 binds to wild-type ULK1 with a binding affinity in the nanomole range (K D =291.4 nM). LYN-1604 (0.5, 1.0 and 2.0 μM) induces cell death via the ULK complex in MDA-MB-231 cells. LYN-1604 (0.5-2 μM, 24 hours) induces remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II in MDA-MB-231 cells. LYN-1604 induces ATG5-dependent autophagy via the ULK complex. LYN-1604 can also increase cleavage of caspase3 and induce apoptosis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MDA-MB-231 cells Concentration: 0.5, 1.0 and 2.0 μM Incubation Time: Result: Induced cell death. Autophagy ratio was increased in a dose-dependent manner. Western Blot AnalysisCell Line: MDA-MB-231 cells Concentration: 0, 0.5, 1, and 2 μM Incubation Time: 24 hours Result: Induced remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II. In Vivo LYN-1604 (low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg; intragastric administration once a day for 14 days) inhibits the growth of xenograft TNBC by targeting ULK1-modulated cell death . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 24 female nude mice (BALB/c, 6-8 weeks, 20-22 g) Dosage: Low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg Administration: Intragastric administration; once a day for 14 days Result: Significantly inhibited the growth of xenograft MDA-MB-231 cells. The body weights of mice were stable. By the end of the experiment, the liver and spleen weight indexes of mice were slightly increased in parts of the groups, while the kidney weight index was not affected in all dose groups. Form:Solid IC50& Target:ULK1 18.94 nM (EC 50 )
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LYN-1604 dihydrochloride
CAS number：2310109-38-5 molecular formula：C33H45Cl4N3O2
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| Chinese alias | LYN-1604 二盐酸盐 | ||
| English alias | - | ||
| CAS number | 2310109-38-5 | molecular formula | C33H45Cl4N3O2 |
| molecular weight | 657.54 g/mol | Exact mass | ≥99% |
| PSA | 36.000 Ų | logp | - |
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