Bestatin (NK421)

Catalog No.S1591 Synonyms: Ubenimex

For research use only.

Bestatin (NK421, Ubenimex) is a potent aminopeptidase-B and leukotriene (LT) A4 hydrolase inhibitor, used in the treatment of acute myelocytic leukemia.

Bestatin (NK421) Chemical Structure

CAS No. 58970-76-6

Selleck's Bestatin (NK421) has been cited by 6 Publications

1 Customer Review

Purity & Quality Control

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Biological Activity

Description Bestatin (NK421, Ubenimex) is a potent aminopeptidase-B and leukotriene (LT) A4 hydrolase inhibitor, used in the treatment of acute myelocytic leukemia.
Targets
Aminopeptidase-N [6]
In vitro

Bestatin inhibits proliferation of all the human leukemic cell lines except KG1. Bestatin induces DNA fragmentation quantitatively and DNA ladder and enhances caspase-3 activity in U937 cells. Bestatin dose-dependently induces DNA fragmentation in human leukemic cell lines. [1] Bestatin dose-dependently inhibits the invasion of SN12M cells into reconstituted basement membrane (Matrigel). Bestatin inhibits the degradation of type IV collagen by tumor cells, but not by tumor-conditioned medium (TCM), in a concentration-dependent manner. Bestatin inhibits hydrolysing activities towards substrates of aminopeptidases in SN12M cells. [2] Bestatin inhibits the tube-like formation of human umbilical vein endothelial cells (HUVECs) in vitro. [3] Bestatin exerts a direct stimulating effect on lymphocytes (and monocytes) via its fixation on cell surface leucine-aminopeptidase, and an indirect effect on monocytes (and lymphocytes) via aminopeptidase B inhibition of tuftsin catabolism. [4]

In vivo Bestatin significantly inhibits the melanoma cell-induced angiogenesis in a mouse dorsal air sac assay. Bestatin reduces the number of vessels oriented towards the established primary tumor mass on the dorsal side of mice implantated of B16-BL6 melanoma cells. [3] Bestatin statistically significantly inhibits leukotriene B4 biosynthesis in the esophageal tissues of EGDA rats and reduces the incidence of EAC in the EGDA rats from 57.7% (15 of 26 rats) to 26.1% (6 of 23 rats). [5]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 0.4 mg/mL
(1.29 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 308.37
Formula

C16H24N2O4

CAS No. 58970-76-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)CC(C(=O)O)NC(=O)C(C(CC1=CC=CC=C1)N)O

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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