Bestatin (Ubenimex)

Description: Bestatin (also called Ubenimex) is a potent, naturally occuring and broad-spectrum aminopeptidase-B and leukotriene (LT) A4 hydrolase inhibitor, it is used in the treatment of acute myelocytic leukemia. Bestatin is isolated from the culture filtrate of Streptomyces olivoreticuli MD976-C7. The structure of bestatin was elucidated to be (2S, 3R)-3-amino-2-hydroxy-4- phenylbutanoyll-(S)-leucine. Bestatin itself was not hydrolyzed by either of the enzymes, when bestatin was incubated as substrate, L-leucine was not detected by thin-layer chromatography. 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.

References: Leukemia. 1999 May; 13(5):729-34; Clin Exp Metastasis. 1992 Jan; 10(1):49-59; Cancer Lett. 2004 Dec 8; 216(1):35-42.

Related CAS: 223763-80-2 (TFA salt); 65391-42-6 (HCl); 339186-54-8 (Bestatin-amido-Me)