Ubenimex
Ubenimex, also known as bestatin, is a dipeptide inhibitor of aminopeptidases such as aminopeptidase N/CD13. Bestatin displays efficacy in the treatment of lung cancer. This compound exhibits anticancer chemotherapeutic, immunomodulatory, and analgesic activities. Bestatin enhances differentiation of acute promyelotic leukemia (APL) cells. Additionally, bestatin enhances proliferation of bone marrow macrophage progenitor cells and formation of CFU-GM colonies. This compound also inhibits catabolism of opioid endopeptides.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18978611
| Cas No. |
58970-76-6 |
|---|---|
| Purity |
≥98% |
| Formula |
C16H24N2O4 |
| Formula Wt. |
308.37 |
| Chemical Name |
N-[(2S,3R)-3-Amino-2-hydroxy-1-oxo-4phenylbutyl]-L-leucine |
| IUPAC Name |
(2S)-2-[[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]amino]-4-methylpentanoic acid |
| Synonym |
Bestatin |
| Melting Point |
233-236°C |
| Solubility |
Soluble in acetic acid, DMSO and methanol. Less soluble in water. Insoluble in ethyl acetate, benzene, hexane and chloroform. |
| Appearance |
White to off white powder |
Hitzerd SM, Verbrugge SE, Ossenkoppele G, et al. Positioning of aminopeptidase inhibitors in next generation cancer therapy. Amino Acids. 2014 Apr;46(4):793-808. PMID: 24385243.
Qian X, He J, Zhao Y, et al. Inhibition of p38 MAPK Phosphorylation Is Critical for Bestatin to Enhance ATRA-Induced Cell Differentiation in Acute Promyelocytic Leukemia NB4 Cells. Am J Ther. 2013 Oct 17. [Epub ahead of print]. PMID: 24141198.
Jia MR, Wei T, Xu WF. The Analgesic Activity of Bestatin as a Potent APN Inhibitor. Front Neurosci. 2010 Jun 28;4:50. PMID: 20631848.
