LYN-1604 dihydrochloride 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 dihydrochloride 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 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 50 mg/mL(76.04 mM;Need ultrasonic) DMSO : 50 mg/mL(76.04 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.5208 mL | 7.6041 mL | 15.2082 mL | | 5 mM | 0.3042 mL | 1.5208 mL | 3.0416 mL | | 10 mM | 0.1521 mL | 0.7604 mL | 1.5208 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (3.80 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.80 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (3.80 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.80 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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