LYN-1604 是一种有效的 UNC-51 样激酶 1 (ULK1) 激活剂，EC50值为 18.94 nM。LYN-1604 可用于三阴性乳腺癌 (TNBC) 的研究。
| 生物活性 | LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breastcancer(TNBC)[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | LYN-1604 is a potential ULK1 agonist (enzymatic activity=195.7% at 100 nM and IC50=1.66 μM against MDA-MB-231 cells)[1].
LYN-1604 binds to wild-type ULK1 with a binding affinity in the nanomole range (KD=291.4 nM)[1].
LYN-1604 (0.5, 1.0 and 2.0 μM) induces cell death via the ULK complex in MDA-MB-231 cells[1].
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[1].
LYN-1604 induces ATG5-dependent autophagy via the ULK complex[1].
LYN-1604 can also increase cleavage of caspase3 and induce apoptosis[1].
Cell Viability Assay[1] | Cell 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 Analysis[1] | Cell 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. |
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体内研究
(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[1].
| Animal Model: | 24 female nude mice (BALB/c, 6-8 weeks, 20-22 g)[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(171.05 mM;Need ultrasonic and warming) 配制储备液 | 1 mM | 1.7105 mL | 8.5526 mL | 17.1051 mL | | 5 mM | 0.3421 mL | 1.7105 mL | 3.4210 mL | | 10 mM | 0.1711 mL | 0.8553 mL | 1.7105 mL |
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