计算溶液所需的质量、体积或浓度。
提供 ≥95% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC 50 of 24.5 µM and a K d of 16 µM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo
In Vitro
LV-320 (0-120 µM; SKBR3, MCF7, JIMT1, and MDA-MB-231 cells) treatment results in a dose-dependent increase in endogenous LC3B-II and protein p62 levels in all four cell lines. LV-320 (120 µM; 48 hours; MDA-MB-231 cells) treatment results in an increase in LC3B-II, indicating that LV-320 blocks autophagic flux. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: SKBR3, MCF7, JIMT1, and MDA-MB-231 cells Concentration: 0 µM, 25 µM, 50 µM, 75 µM, 100 µM, or 120 µM Incubation Time: Result: Resulted in a dose-dependent increase in endogenous LC3B-II and protein p62 levels in all four cell lines. Cell Autophagy AssayCell Line: MDA-MB-231 cells Concentration: 120 µM Incubation Time: 48 hours Result: Blocked autophagic flux.
In Vivo
LV-320 (100-200 mg/kg; oral gavage; three times over two days; GFP-LC3 mice) treatment results in a terminal blood level of 169 µM and a liver level of 104 µM. The expression of GFP-LC3 puncta is significantly greater accumulation in LV-320 treated animals compared to controls. LC3B-II protein is also increased in LV-320-treated animals. The treatment do not cause significant toxicity in mice at either dose . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: GFP-LC3 mice (females, 9-14 weeks) Dosage: 100 mg/kg or 200 mg/kg Administration: Oral gavage; three times over two days (Pharmacokinetic study) Result: Terminal blood levels were 169 µM and liver levels were 104 µM. LC3B-II protein level was also increased.
Form:Solid
IC50& Target:IC50: 24.5 µM (ATG4B),Kd: 16 μM (ATG4B)
分类树(Taxonomy Tree)
| 界(kingdom) | 有机化合物 |
|---|---|
| 超类(Superclass) | 有机杂环化合物 |
| 类(Class) | 喹啉及其衍生物 |
| 亚类(Subclass) | 卤代喹啉 |
| 中间层级节点(Intermediate Tree Nodes) | 暂无 |
| 直接上位类(Direct Parent) | 卤代喹啉 |
| 其他上位类(Alternative Parents) | 羟基吡啶 苯及其取代衍生物 杂芳族化合物 亚磺酰基化合物 一元羧酸及其衍生物 二烷基硫醚 羧酸 氮杂环化合物 有机光子化合物 有机氧化合物 有机氮化合物 有机氯化物 有机氧化物 碳氢化合物衍生物 |
| 分子骨架(Molecular Framework) | 芳香族杂多环化合物 |
| 取代基(Substituents) | 芳香族杂多环化合物 - 氮杂环 - 苯基化合物 - 羧酰胺基 - 羧酸衍生物 - 二烷基硫醚 - 卤喹啉 - 杂芳香族化合物 - 烃衍生物 - 羟基吡啶 - 单羧酸或其衍生物 - 单环苯基基团 - 有机硝基化合物 - 有机氧化物 - 有机氧化合物 - 有机氯化物 - 有机卤化物 - 有机氮化合物 - 有机氧化合物 - 有机氮化合物 - 有机硫化合物 - 吡啶 - 硫酰基化合物 - 硫醚 |
| 描述(Description) | 该化合物属于有机化合物中的卤代喹啉类。这类化合物含有喹啉骨架,其环上一个或多个位置被n个卤素原子取代。 |
| 外部描述符(External Descriptors) | 暂无 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|