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Bestatin hydrochloride

Catalog No. T3529   CAS 65391-42-6
Synonyms: 苯丁抑制素, 盐酸乌苯美司, Ubenimex hydrochloride

Bestatin (Ubenimex) hydrochlorideis an inhibitor of aminopeptidase N (APN)/CD13 and aminopeptidase B.

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Bestatin hydrochloride, CAS 65391-42-6
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Bestatin (Ubenimex) hydrochlorideis 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.
Synonyms 苯丁抑制素, 盐酸乌苯美司, Ubenimex hydrochloride
Molecular Weight 344.84
Formula C16H25ClN2O4
CAS No. 65391-42-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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. 2. Qian X, et al. Inhibition of p38 MAPK Phosphorylation Is Critical for Bestatin to Enhance ATRA-Induced Cell Differentiation in Acute Promyelocytic Leukemia NB4 Cells. Am J Ther. 2016 May-Jun;23(3):e680-9. 3. Lis M, et al. The effects of bestatin on humoral response to sheep erythrocytes in non-treated and cyclophosphamide-immunocompromised mice. Immunopharmacol Immunotoxicol. 2013 Feb;35(1):133-8. 4. Poloz Y, et al. Bestatin inhibits cell growth, cell division, and spore cell differentiation in Dictyostelium discoideum. Eukaryot Cell. 2012 Apr;11(4):545-57. 5. Zhu X, Liu S, Wang X, et al. Contribution of porcine aminopeptidase N to porcine deltacoronavirus infection[J]. Emerging microbes & infections. 2018 Apr 11;7(1):65.

Citations

1. Zhu X, Liu S, Wang X, et al. Contribution of porcine aminopeptidase N to porcine deltacoronavirus infection. Emerging Microbes & Infections. 2018 Apr 11;7(1):65

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Hematonosis Compound Library Drug-induced Liver Injury (DILI) Compound Library Anti-Metabolism Disease Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Cytoskeletal Signaling Pathway Compound Library Approved Drug Library Anti-Cancer Drug Library

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DG051 Methyl arachidate Tosedostat α-Cyclopentyl-4-(2-quinolinylmethoxy)benzeneacetic acid L(+)-Leucinol Acebilustat Bestatin hydrochloride Betulinic acid

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Keywords

Bestatin hydrochloride 65391-42-6 代谢 微生物学 细胞骨架 Aminopeptidase Antibacterial Antibiotic Integrin Bestatin Inhibitor Bacterial inhibit Ubenimex hydrochloride Ubenimex inhibitor