亮肽素 T6564

Product Introduction
Bioactivity


英文名: Leupeptin Hemisulfate

描述: Leupeptin hemisulfate 是一种蛋白酶抑制剂，具有细胞膜渗透性、可逆性、竞争性和口服活性。Leupeptin hemisulfate 可以抑制 Cathepsin B、Cathepsin H、Cathepsin L 的活性，阻断两性溶酶体的融合。Leupeptin hemisulfate 还具有抗炎活性。

激酶实验: Determination of BET Protein Binding Affinities to I-BET726: For determination of binding affinities to BET protein bromodomains, I-BET726 is titrated against truncates containing both BD1 and BD2 of BRD2 (10 nM), BRD3 (10 nM), and BRD4 (10 nM) in 50 mM HEPES pH7.5, 150 mM NaCl, 5% Glycerol, 1 mM DTT and 1 mM CHAPS in the presence of an Alexa 647 derivative (50 nM) of fluorescent ligand. After equilibrating for 1 h, the bromodomain protein: ligand interaction is detected using Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET) following the addition of 1.5 nM europium chelate labeled anti-6His antibody. Plates are read using an Envision Plate reader (λEX = 337 nm, λEM = 615 nm, λEM = 665 nm; dual dichroic = 400 nm & 630 nm). These data are fitted to a four parameter IC50 model using Graphit data analysis software.

体外活性: 方法：SARS-CoV-2 感染的 Vero 细胞用 Leupeptin hemisulfate (0.06-200 µM) 处理 72 h，使用 RT-PCR 检测病毒 RNA 水平。结果：Leupeptin hemisulfate 可以抑制 Vero 细胞中 SARS-CoV-2 的 RNA 水平，EC50 值为 42.34  µM。[1]方法：SARS-CoV-2 假病毒感染的 Huh7 细胞用 Leupeptin hemisulfate (0.1-100 µM) 处理 24 h，使用 luciferase activity assay 检测假病毒感染情况。结果：Leupeptin hemisulfate 抑制 Vero 细胞中的假病毒感染，EC50 值为 39.29  µM。[2]

体内活性: 方法：为测定巨噬细胞自噬通量，将 Leupeptin hemisulfate (9-40 mg/kg in 0.5 mL PBS) 单次腹腔注射给 C57BL/6NCrl 小鼠。结果：Leupeptin hemisulfate 治疗后 LC3b 的积累率在肝脏最高，在脾脏最低。LC3a、ATG8/LC3b 同源物和 LC3b 相互作用蛋白 p62 以与 LC3b 相似的动力学降解。[3]方法：为检测寒冷是否激活自噬流量，将 Leupeptin hemisulfate (40 mg/kg) 单次腹腔注射给 C57B6 小鼠，1 h 后将小鼠在 4 ℃ 下冷暴露 1 h。结果：冷暴露小鼠在棕色脂肪中的 LC3-II 通量增加了 >2 倍。[4]

存储条件: keep away from moisturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 87 mg/mL (182.9 mM)
DMSO : 60 mg/mL (126.16 mM)
Ethanol : 88 mg/mL (185 mM)


关键字: inhibit | Cathepsin | Leupeptin Hemisulfate | Inhibitor | Leupeptin

相关产品: Alvelestat | ML281 | AE-3763 | Patamostat HCl | Sivelestat | JCP174 | Gabexate mesylate | Upamostat | Chrysophanol 8-O-glucoside | SC-514

相关库: Anti-Tumor Natural Product Library | Oxidation-Reduction Compound Library | Bioactive Compounds Library Max | Peptide Compound Library | Inhibitor Library | Anti-Fibrosis Compound Library | Natural Product Library for HTS | Microbial Natural Product Library | Target-Focused Phenotypic Screening Library | Covalent Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途