Bestatin hydrochloride
(Synonyms: 盐酸乌苯美司; Ubenimex hydrochloride) 目录号 : GC15577
An aminopeptidase inhibitor
Cas No.:65391-42-6
Sample solution is provided at 25 µL, 10mM.
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Bestatin hydrochloride, also known as Ubenimex, is an inhibitor of aminopeptidase B and N (APN)/CD13 [1].
Bestatin, an antibiotic of microbial origin, is a potent inhibitor of some aminopeptidases which can be administered to cultured cells, intact animals and humans with low toxicity. It has been used as an useful tool to assess the physiological role of certain mammalian exopeptidases in the regulation of the immune system, the growth of tumors and their invasion of surrounding tissues, and the degradation of cellular proteins [2].
In vivo: In a mouse dorsal air sac assay, oral administration of bestatin (100-200 mg/kg/day) showed a significant inhibitory activity against the melanoma cell-induced angiogenesis. Bestatin also inhibited the tube-like formation of human umbilical vein endothelial cells (HUVECs). Furthermore, after the orthotopic implantation of B16-BL6 melanoma cells into mice, bestatin administration (50-100 mg/kg/day, i.p) reduced the number of vessels oriented towards the established primary tumor mass on the dorsal side of mice [1].
References:
[1]. Aozuka Y1, Koizumi K, Saitoh Y, Ueda Y, Sakurai H, Saiki I. Anti-tumor angiogenesis effect of aminopeptidase inhibitor bestatin against B16-BL6 melanoma cells orthotopically implanted into syngeneic mice. Cancer Lett. 2004 Dec 8;216(1):35-42.
[2]. Scornik OA1,Botbol V.Bestatin as an experimental tool in mammals. Curr Drug Metab.2001 Mar;2(1):67-85.
| Cell experiment [1]: | |
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Cell lines |
D. discoideum cells, human umbilical vein endothelial cells |
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Preparation method |
Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
600 μM, 48 h |
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Applications |
Bestatin (600 μM)-treated cells progressed slower through the cell cycle due to decreased rate of cell growth and the frequency of cell division. Bestatin inhibited the frequency of mitosis and the inherent multinuclearity in D. discoideum cells, and was not cytotoxic to D. discoideum cells at 0-600 μM. Bestatin inhibited aminopeptidase activity in lysates of PsaA-GFP- and GFP-expressing cells by 69.39% ± 10.5% and 39.93% ± 18.7% of control, respectively. Bestatin (1-100 μg/ml) dose-dependently inhibited the Ala-MCA-hydrolysing activity of HUVECs. Bestatin inhibited the tube-like formation of HUVECs. |
| Animal experiment [2]: | |
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Animal models |
Inbred 6-week-old female C57BL/6 mice bearing B16-BL6 melanoma xenografts |
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Dosage form |
Oral administration, 100-200 mg/kg/day; Intraperitoneal injection, 50-100 mg/kg/day |
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Application |
In a mouse dorsal air sac assay, oral administration of bestatin (100-200 mg/kg/day) significantly inhibited melanoma cell-induced angiogenesis. After the orthotopic implantation of B16-BL6 melanoma cells into mice, bestatin administration (50-100 mg/kg/day, i.p.) reduced the number of vessels oriented towards the established primary tumor mass on the dorsal side of mice. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Poloz Y, Catalano A, O'Day D H. Bestatin inhibits cell growth, cell division, and spore cell differentiation in Dictyostelium discoideum[J]. Eukaryotic cell, 2012, 11(4): 545-557. [2]. Aozuka Y, Koizumi K, Saitoh Y, et al. Anti-tumor angiogenesis effect of aminopeptidase inhibitor bestatin against B16-BL6 melanoma cells orthotopically implanted into syngeneic mice[J]. Cancer letters, 2004, 216(1): 35-42. |
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| Cas No. | 65391-42-6 | SDF | |
| 别名 | 盐酸乌苯美司; Ubenimex hydrochloride | ||
| 化学名 | (2S)-2-[[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]amino]-4-methylpentanoic acid;hydrochloride | ||
| Canonical SMILES | CC(C)CC(C(=O)O)NC(=O)C(C(CC1=CC=CC=C1)N)O.Cl | ||
| 分子式 | C16H25ClN2O4 | 分子量 | 344.83 |
| 溶解度 | ≥ 125 mg/mL in DMSO, ≥ 34.2 mg/mL in Water, ≥ 68 mg/mL in EtOH | 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 | 2.9 mL | 14.4999 mL | 28.9998 mL |
| 5 mM | 0.58 mL | 2.9 mL | 5.8 mL |
| 10 mM | 0.29 mL | 1.45 mL | 2.9 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet