For research use only.
Catalog No.S1591 Synonyms: Ubenimex
CAS No. 58970-76-6
Bestatin (NK421, Ubenimex) is a potent aminopeptidase-B and leukotriene (LT) A4 hydrolase inhibitor, used in the treatment of acute myelocytic leukemia.
Selleck's Bestatin (NK421) has been cited by 5 publications
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|Description||Bestatin (NK421, Ubenimex) is a potent aminopeptidase-B and leukotriene (LT) A4 hydrolase inhibitor, used in the treatment of acute myelocytic leukemia.|
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.  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.  Bestatin inhibits the tube-like formation of human umbilical vein endothelial cells (HUVECs) in vitro.  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. 
|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.  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). |
-  Sekine K, et al. Leukemia, 1999, 13(5), 729-734.
-  Yoneda J, et al. Clin Exp Metastasis, 1992, 10(1), 49-59.
-  Aozuka Y, et al. Cancer Lett, 2004, 216(1), 35-42.
|In vitro||DMSO||0.4 mg/mL (1.29 mM)|
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