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Bestatin

Catalog No. T1257 CAS 58970-76-6

Synonyms: Ubenimex

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

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Bestatin, CAS 58970-76-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 48.00
10 mg	In stock	$ 65.00
25 mg	In stock	$ 112.00
50 mg	In stock	$ 177.00
100 mg	In stock	$ 293.00
500 mg	In stock	$ 728.00

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Purity: 100%

Purity: 99.63%

Purity: 99.35%

Purity: 99.02%

Purity: 98%

Biological Description

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Description	Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.
In vitro	In mice bearing B16-BL6 melanoma tumors on their dorsolateral sides, Bestatin reduced the number of blood vessels in established primary tumor masses. Additionally, Bestatin significantly inhibited angiogenesis induced by melanoma cells in the dorsal air sac assay in mice. In EGDA rats, Bestatin decreased the incidence of EAC from 57.7% to 26.1%. Moreover, Bestatin demonstrated statistically significant inhibition of leukotriene B4 biosynthesis in the esophageal tissues of EGDA rats.
In vivo	Bestatin exhibits a concentration-dependent inhibition of SN12M cell invasion into reconstituted basement membrane (matrigel). It also concentration-dependently inhibits the degradation of type IV collagen by tumor cells in a non-neoplastic condition medium. In U937 cells, bestatin enhances the activity of caspase-3, inducing DNA laddering and fragmentation. Additionally, in SN12M, bestatin inhibits the hydrolytic activity of aminopeptidase substrates. Furthermore, bestatin inhibits tube formation in human umbilical vein endothelial cells. Through binding to leucine aminopeptidase fixed on the cell surface, bestatin directly stimulates lymphocytes (and monocytes), whereas it indirectly does so by impeding the degradation metabolism of the phagocytosis stimulating hormones through the inhibition of aminopeptidase B.
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	Ubenimex
Molecular Weight	308.37
Formula	C16H24N2O4
CAS No.	58970-76-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

1eq. NaOH: 15.4 mg/mL (50 mM)

References and Literature

1. Sekine K, et al. Leukemia, 1999, 13(5), 729-734. 2. Yoneda J, et al. Clin Exp Metastasis, 1992, 10(1), 49-59. 3. Aozuka Y, et al. Cancer Lett, 2004, 216(1), 35-42. 4. Mathé G, et al. Biomed Pharmacother, 1991, 45(2-3), 49-54. 5. Chen X, et al. J Natl Cancer Inst, 2003, 95(14), 1053-1061. 6. Jiang T Y, Feng X F, Fang Z, et al. PTEN deficiency facilitates the therapeutic vulnerability to proteasome inhibitor bortezomib in gallbladder cancer[J]. Cancer Letters. 2020 7. Jiang T Y, Pan Y F, Wan Z H, et al. PTEN status determines chemosensitivity to proteasome inhibition in cholangiocarcinoma[J]. Science Translational Medicine. 2020, 12(562).

Citations

1. Jiang T Y, Pan Y F, Wan Z H, et al. PTEN status determines chemosensitivity to proteasome inhibition in cholangiocarcinoma. Science Translational Medicine. 2020, 12(562). 2. Jiang T Y, Feng X F, Fang Z, et al. PTEN deficiency facilitates the therapeutic vulnerability to proteasome inhibitor bortezomib in gallbladder cancer. Cancer Letters. 2021, 501: 187-199.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Microbial Natural Product Library Anti-infective Natural Product Library Anti-Viral Compound Library NO PAINS Compound Library

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Tosedostat Methyl arachidate Betulinic acid L(+)-Leucinol Aminopeptidase-IN-1 SC-22716 ARM1 Acebilustat

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Keywords

Bestatin 58970-76-6 Immunology/Inflammation Metabolism Microbiology/Virology Others Aminopeptidase Antibacterial Antibiotic LTR Bacterial Inhibitor Ubenimex inhibit inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.