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Bestatin hydrochloride

现货
Catalog No.
A8621
氨肽酶N(APN/CD13)和氨肽酶B抑制剂。
组合的产品项目
规格价格库存 数量
5mg
¥ 500.00
现货
10mg
¥ 700.00
现货
25mg
¥ 1,200.00
现货
100mg
¥ 3,400.00
现货

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Background

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.

Chemical Properties

StorageStore at -20°C
M.Wt344.83
Cas No.65391-42-6
FormulaC16H25ClN2O4
Solubility≥125 mg/mL in DMSO, ≥34.2 mg/mL in H2O, ≥68 mg/mL in EtOH
Chemical Name(2S)-2-[[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]amino]-4-methylpentanoic acid;hydrochloride
SDFDownload SDF
Canonical SMILESCC(C)CC(C(=O)O)NC(=O)C(C(CC1=CC=CC=C1)N)O.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

D. discoideum细胞,人脐静脉内皮细胞

溶解方法

可溶于DMSO。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

600 μM,48 h

应用

Bestatin(600 μM)通过降低细胞生长速度和细胞分裂频率导致细胞周期进展缓慢。在D. discoideum细胞中,Bestatin抑制有丝分裂的发生频率以及固有的多核性,在0-600 μM浓度下,Bestatin对D. discoideum细胞没有细胞毒性。与对照组相比,Bestatin抑制PsaA-GFP和GFP表达细胞的裂解液中的氨肽酶活性,分别抑制69.39%±10.5%和39.93%±18.7%。Bestatin(1-100 μg/ml)以浓度依赖性方式抑制HUVECs的Ala-MCA水解活性。Bestatin抑制HUVECs的管状形成。

动物实验 [2]:

动物模型

具有B16-BL6黑色素瘤异种移植物的近交6周龄雌性C57BL/6小鼠

给药剂量

口服,100-200 mg/kg/day;腹腔注射,50-100 mg/kg/day

应用

在小鼠背侧气囊实验中,口服给药bestatin(100-200 mg/kg/day)显著抑制黑色素瘤细胞诱导的血管发生。在将B16-BL6黑色素瘤细胞原位植入小鼠后,腹腔注射50-100 mg/kg/day剂量的bestatin减少了小鼠背侧朝着已建立的原发性肿瘤块定向的血管数量。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

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.

质量控制

化学结构

Bestatin hydrochloride