Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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,并且稳定无毒,在体内具有活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 11,759 | 6-8周 | ||
50 mg | ¥ 18,700 | 6-8周 | ||
100 mg | ¥ 26,437 | 6-8周 |
产品描述 | 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. These findings suggest that LV-320 will serve as a relevant chemical tool to study the various roles of ATG4B in cancer and other contexts [1]. |
靶点活性 | ATG4B:(kd)16 μM , ATG4B:24.5 µM |
体外活性 | LV-320 (0-120 μM; SKBR3, MCF7, JIMT1, and MDA-MB-231 cells) treatment leads to 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]. 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. |
体内活性 | LV-320 (100-200 mg/kg; oral gavage; three times over two days; GFP-LC3 mice) treatment leads to 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]. 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 |
分子式 | C29H26ClNO2S2 |
CAS No. | 2449093-46-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 135 mg/mL (259.56 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9227 mL | 9.6134 mL | 19.2267 mL | 48.0668 mL |
5 mM | 0.3845 mL | 1.9227 mL | 3.8453 mL | 9.6134 mL | |
10 mM | 0.1923 mL | 0.9613 mL | 1.9227 mL | 4.8067 mL | |
20 mM | 0.0961 mL | 0.4807 mL | 0.9613 mL | 2.4033 mL | |
50 mM | 0.0385 mL | 0.1923 mL | 0.3845 mL | 0.9613 mL | |
100 mM | 0.0192 mL | 0.0961 mL | 0.1923 mL | 0.4807 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
LV-320 2449093-46-1 Proteases/Proteasome Cysteine Protease LV 320 LV320 Inhibitor inhibitor inhibit