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.
Nan Fang Yi Ke Da Xue Xue Bao. 2020 Oct 30;40(10):1465-1471.
Pathogenic role leukotriene B4 in lung injury induced by lung-protective mechanical ventilation in rabbits
Ubenimex purchased from AbMole
|Source||Nan Fang Yi Ke Da Xue Xue Bao (2020 Oct), Figure 3, Ubenimex (Abmole Bioscience)|
|Cell Lines||Japanese white rabbits|
|Incubation Time||5 days|
|Results||Compared with those in PM group, the rabbits in group BPM showed significantly reduced LTB4 production in the lungs (P < 0.05), up-regulated cAMP/ PKA and Rap1 signaling pathway activities (P < 0.05), and alleviated lung hyper-permeability and inflammation (P < 0.05).|
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO 3 mg/mL|
|Related Aminopeptidase Products|
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Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
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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