Ubenimex (Bestatin) is an inhibitor of aminopeptidase B, leukotriene A4 hydrolase, aminopeptidase N (Ki = 0.001 - 90 mM). Ubenimex inhibits enkephalin metabolism and leukotriene A4 hydrolase. Bestatin also inhibits tumor cell proliferation. Bestatin induced cell growth inhibition and phenotypic changes of HL-60 and HL-60R cell lines. In vitro, the upregulation of CD13/aminopeptidase N was found after 1 hr, however, the downregulation was observed after 3 hrs incubation with Ubenimex (Bestatin). On the other hand, the downregulation of CD15 and CD33 was observed after both one and 3 hrs incubation. Ubenimex may also be an effective anti-leukemic agent in vivo.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Effect of ubenimex (Bestatin) on the cell growth and phenotype of HL-60 and HL-60R cell lines: up-and down-regulation of CD13/aminopeptidase N.
Imamura N, et al. Leuk Lymphoma. 2000 May;37(5-6):663-7. PMID: 11042531.
|Related Aminopeptidase Products|
CHR-2797 is an aminopeptidase inhibitor for LAP, PuSA and Aminopeptidase N with IC50 of 100 nM, 150 nM and 220 nM, respectively.
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