LV-320

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LV-320  纯度: ≥95.0%

LV-320 是一种有效且非竞争性的 ATG4B 抑制剂，其 IC50 值为 24.5 μM，Kd 值为 16 μM。 LV-320 抑制 ATG4B 的酶促活性，阻断细胞自噬，并且在体内稳定，无毒且有活性。

LV-320

LV-320 Chemical Structure

CAS No. : 2449093-46-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5149 In-stock
5 mg ￥4500 In-stock
10 mg ￥7500 In-stock
50 mg ￥22500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

LV-320 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library

生物活性

LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5 µM and a Kd of 16 µM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo[1].

IC50 & Target

IC50: 24.5 µM (ATG4B); Kd: 16 μM (ATG4B)[1]
体外研究
(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[1].
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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell 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 Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 120 µM
Incubation Time: 48 hours
Result: Blocked autophagic flux.

体内研究
(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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: GFP-LC3 mice (females, 9-14 weeks)[1]
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.

分子量

520.11

Formula

C29H26ClNO2S2
CAS 号

2449093-46-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 135 mg/mL (259.56 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9227 mL 9.6134 mL 19.2267 mL
5 mM 0.3845 mL 1.9227 mL 3.8453 mL
10 mM 0.1923 mL 0.9613 mL 1.9227 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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: ≥ 2.25 mg/mL (4.33 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (4.33 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 22.5 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.25 mg/mL (4.33 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (4.33 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 22.5 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Bosc D, et al. A new quinoline-based chemical probe inhibits the autophagy-related cysteine protease ATG4B. Sci Rep. 2018 Aug 3;8(1):11653. doi: 10.1038/s41598-018-29900-x.

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