Bestatin

SKU: orb1708791

Description

Bestatin

Research Area

Immunology & Inflammation, Infectious Disease & Virology, Metabolism Research

Key Properties

• CAS Number: 58970-76-6
• MW: 308.3728
• Purity: >99.99% (May vary between batches)
• Formula: C₁₆H₂₄N₂O₄
• SMILES: CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)CC1=CC=CC=C1)C(O)=O
• Target: Aminopeptidase,LTR,Antibiotic,Antibacterial
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:0.5 mg/mL (1.62 mM);1eq. NaOH:15.4 mg/mL (49.94 mM);DMSO:10 mg/mL (32.43 mM)

Bioactivity

• 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.
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• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bestatin, Bacterial, APN, Antibiotic, Aminopeptidase, inhibit, Inhibitor, LTA(4)H-h, Ubenimex

Compound Identifiers

PubChem CID

72172