Bestatin

＞98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

乌苯美司；Ubenimex

白色粉末

DMSO : 6 mg/mL (19.46 mM; Need warming)

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

Aminopeptidase-N

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.

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).

[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] Math?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.