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Bestatin HCl

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Chemical Structure| 65391-42-6 同义名 : 盐酸乌苯美司 ;Ubenimex hydrochloride;Bestatin (hydrochloride);Bestatin hydrochloride
CAS号 : 65391-42-6
货号 : A459084
分子式 : C16H25ClN2O4
纯度 : 98%
分子量 : 344.834
MDL号 : MFCD00058004
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(724.99 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(289.99 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Bestatin Hydrochloride is a hydrochloride form of Bestatin. Bestatin is a potent inhibitor of aminopeptidases. The Ki values for bestatin against leucyl aminopeptidase, tripeptide aminopeptidase, cytosol alanyl aminopeptidase, leukotriene A4 hydrolase, aminopeptidase B and nardilysin were 1nM, 0.5μM, 14nM, 0.17μM, 1μM and 15μM, respectively[3]. Pre-incubation of human leukocyte LTA4 hydrolase with 1, 10, or 100μM bestatin resulted in 20%, 50%, and 90% inhibition of [3H]LTA4 labeling of LTA4 hydrolase, respectively. Bestatin inhibited LTB4 formation by LTA4 hydrolase in a dose-dependent manner with 50% inhibition of activity at 10μM[4]. In human umbilical vein endothelial cells (HUVECs), bestatin at 1-100mg/ml inhibited the Ala-MCA-hydrolysing activity of cells in a dose-dependent manner. Bestatin at the same concentration range also resulted in the formation of shorter branching structures in HUVECs compared to the controls. In C57BL/6 mice implanted with B16-BL6 melanoma cells into the dorsal side, intraperitoneal administration of bestatin (50 or 100 mg/kg/day) for 5 days significantly reduced the number of vessels oriented towards the tumor mass without affecting the tumor volume[5].
作用机制 Bestatin is a potent aminopeptidase inhibitor. It competes with the substrates via binding to the catalytic site of the enzyme[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.90mL

0.58mL

0.29mL

14.50mL

2.90mL

1.45mL

29.00mL

5.80mL

2.90mL
参考文献

[1]Hossain A, Heron D, et al. Protective effects of bestatin in the retina of streptozotocin-induced diabetic mice. Exp Eye Res. 2016 Aug;149:100-106.

[2]Poloz Y, Catalano A, O'Day DH. Bestatin inhibits cell growth, cell division, and spore cell differentiation in Dictyostelium discoideum. Eukaryot Cell. 2012 Apr;11(4):545-57.

[3]Scornik OA, Botbol V. Bestatin as an experimental tool in mammals. Curr Drug Metab. 2001 Mar;2(1):67-85. doi: 10.2174/1389200013338748.

[4]Evans JF, Kargman S. Bestatin inhibits covalent coupling of [3H]LTA4 to human leukocyte LTA4 hydrolase. FEBS Lett. 1992 Feb 3;297(1-2):139-42. doi: 10.1016/0014-5793(92)80345-h.

[5]Aozuka Y, 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.

[6]Scornik OA, Botbol V. Bestatin as an experimental tool in mammals. Curr Drug Metab. 2001 Mar;2(1):67-85. doi: 10.2174/1389200013338748.