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Bestatin hydrochloride

Bestatin hydrochloride
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Purity:100%
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Bestatin hydrochloride

Catalog No. T3529Cas No. 65391-42-6
Bestatin hydrochloride (Ubenimex hydrochloride) is an inhibitor of aminopeptidase N (APN)/CD13 and aminopeptidase B.
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Pack SizePriceAvailabilityQuantity
5 mg$47In Stock
10 mg$68In Stock
25 mg$108In Stock
50 mg$177In Stock
100 mg$293In Stock
200 mg$449In Stock
500 mg$728In Stock
1 mL x 10 mM (in DMSO)$52In Stock
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Product Introduction

Bioactivity
Description
Bestatin hydrochloride (Ubenimex hydrochloride) is an inhibitor of aminopeptidase N (APN)/CD13 and aminopeptidase B.
In vitro
Bestatin, also known as Ubenimex (INN), is a competitive protease inhibitor. It is an inhibitor of aminopeptidase B, leukotriene A4 hydrolase, aminopeptidase N. It is being studied for use in the treatment of acute myelocytic leukemia. Bestatin can be administered, with low toxicity, to cultured cells, intact animals and humans. It has become a useful tool in elucidating the physiological role of some mammalian exopeptidases in the regulation of the immune system, in the growth of tumors and their invasion of surrounding tissues, and in the degradation of cellular proteins.
In vivo
Bestatin is an active anti-angiogenic agent that may inhibit tumor angiogenesis in vivo and tube-like formation of endothelial cells in vitro through its inhibition of APN/CD13 activity. Oral administration of Bestatin (100-200 mg/kg/day) is found to significantly inhibit the melanoma cell-induced angiogenesis in a mouse dorsal air sac assay.
Kinase Assay
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 Research
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.
AliasUbenimex hydrochloride
Chemical Properties
Molecular Weight344.84
FormulaC16H25ClN2O4
Cas No.65391-42-6
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 50 mg/mL (144.99 mM)
H2O: 20 mg/mL (58.00 mM)
Solution Preparation Table
DMSO/H2O
1mg5mg10mg50mg
1 mM2.8999 mL14.4995 mL28.9990 mL144.9948 mL
5 mM0.5800 mL2.8999 mL5.7998 mL28.9990 mL
10 mM0.2900 mL1.4499 mL2.8999 mL14.4995 mL
20 mM0.1450 mL0.7250 mL1.4499 mL7.2497 mL
50 mM0.0580 mL0.2900 mL0.5800 mL2.8999 mL
DMSO
1mg5mg10mg50mg
100 mM0.0290 mL0.1450 mL0.2900 mL1.4499 mL

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Preparation method for in vivo formula: Take 50 μLDMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μLTween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify.
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