Bestatin trifluoroacetate
(Synonyms: 乌苯美司三氟乙酸盐; Ubenimex trifluoroacetate) 目录号 : GC35499
An aminopeptidase inhibitor
Cas No.:223763-80-2
Sample solution is provided at 25 µL, 10mM.
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Bestatin is an aminopeptidase inhibitor originally isolated from S. olivoreticuli.1 It inhibits aminopeptidase B (IC50 = 0.05 ?g/ml), aminopeptidase N (IC50 = 16.9 ?M), leucine aminopeptidase (IC50 = 0.01 ?g/ml), and the aminopeptidase activity of leukotriene A4 (LTA4) hydrolase (Kapp = 172 nM).1,2,3 It is selective for these aminopeptidases over aminopeptidase A, trypsin, chymotrypsin, elastase, papain, pepsin, and thermolysin.1 Bestatin inhibits the production of LTB4 in erythrocytes when used at a concentration of 70 ?M.3 It increases the expression of Akt, inhibits proliferation, migration, and invasion, and induces autophagy and apoptosis in 5637 bladder cancer cells.4 Bestatin (5 and 15 mg/kg) decreases serum levels of LTB4 and reduces tumor growth in a patient-derived xenograft (PDX) mouse model of colorectal cancer.5
1.Umezawa, H., Ayoagi, T., Suda, H., et al.Bestatin, an inhibitor of aminopeptidase B, produced by actinomycetesJ. Antibiot. (Tokyo)29(1)97-99(1976) 2.Melzig, M.F., and Bormann, H.Betulinic acid inhibits aminopeptidase N activityPlanta Med.64(7)655-657(1998) 3.?rning, L., Krivi, G., and Fitzpatrick, F.A.Leukotriene A4 hydrolase. Inhibition by bestatin and intrinsic aminopeptidase activity establish its functional resemblance to metallohydrolase enzymesJ. Biol. Chem.266(3)1375-1378(1991) 4.Wang, X., Liu, Y., Liu, W., et al.Ubenimex, an APN inhibitor, could serve as an anti?tumor drug in RT112 and 5637 cells by operating in an Akt?associated mannerMol. Med. Rep.17(3)4531-4539(2018) 5.Zhao, S., Yao, K., Li, D., et al.Inhibition of LTA4H by bestatin in human and mouse colorectal cancerEBioMedicine44361-374(2019)
Kinase experiment: | Cells are harvested, washed, and lysed in NP-40 lysis buffer (50 mM Tris-HCl [pH 7.5], 150 mM NaCl, 0.5% NP-40). Total cell protein is quantified using the Bradford assay and 1-mg/mL protein aliquots are made. Ten microliters of total cell protein is mixed with 290 μL of substrate solution (0.1 mg/mL dithiothreitol [DTT], 0.1 mg/mL albumin, and 1 mM alanine-β-naphthylamide). Fluorometric measurements (340 nm excitation, 400 nm emission) are made after 15 and 30 min. The slope of the line between the 15- and 30-min measurements is used to represent aminopeptidase activity. Total cell protein is preincubated with bestatin, amastatin, puromycin, EDTA, and/or ZnCl2 for 20 min before the fluorometric aminopeptidase assay. |
Cell experiment: | Growing cells (1×106 to 2×106 cells/mL) are diluted to 1.0×103 cells/mL and transferred (3 mL) into a well in a 12-well multiwell plate (2.5-cm diameter/well). Cells are treated with 0, 10, 50, 100, 300, or 600 μM Bestatin and allowed to grow at 21°C shaking at 180 rpm for 48 h. A hemocytometer is used to measure cell density after 0, 24, and 48 h. |
Animal experiment: | Bestatin is dissolved in PBS. The agent (doses of 10, 1, and 0.1 mg/kg) is injected i.p. to non-cyclophosphamide-treated mice, 5 or 10 times at 24-h intervals before SRBC immunization. The mice are immunized 24 h after the last dose of bestatin. Pharmacological immunosuppression is induced by a single intraperitoneal injection of cyclophosphamide administered at a dose of 350 mg/kg, 12 days before SRBC immunization. Bestatin at the doses of 1 and 0.1 mg/kg is injected to cyclophosphamide-immunosuppressed mice i.p. five times at 48-h intervals or 10 times at 24-h intervals before SRBC immunization. The first dose of bestatin is administered 24 h after cyclophosphamide, while the last dose of the drug is injected 24h before SRBC immunization. |
References: [1]. Hossain A, et al. Protective effects of bestatin in the retina of streptozotocin-induced diabetic mice. Exp Eye Res. 2016 Aug;149:100-6 | |
| Cas No. | 223763-80-2 | SDF | |
| 别名 | 乌苯美司三氟乙酸盐; Ubenimex trifluoroacetate | ||
| Canonical SMILES | FC(F)(C(O)=O)F.CC(C)C[C@@H](C(O)=O)NC([C@@H](O)[C@H](N)CC1=CC=CC=C1)=O | ||
| 分子式 | C18H25F3N2O6 | 分子量 | 422.4 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3674 mL | 11.8371 mL | 23.6742 mL |
| 5 mM | 0.4735 mL | 2.3674 mL | 4.7348 mL |
| 10 mM | 0.2367 mL | 1.1837 mL | 2.3674 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet