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. 2017 Nov 20;37(11):1523-1528.
Pathogenic role of leukotriene B4 in pulmonary microvascular endothelial cell hyper- permeability induced by one lung ventilation in rabbits
Ubenimex purchased from AbMole
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
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Source | Nan Fang Yi Ke Da Xue Xue Bao (2020 Oct), Figure 3, Ubenimex (Abmole Bioscience) |
| Method | oral gavage | |
| Cell Lines | Japanese white rabbits | |
| Concentrations | 8 mg/kg·d | |
| 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). |
| Molecular Weight | 308.38 |
| Formula | C16H24N2O4 |
| CAS Number | 58970-76-6 |
| Solubility (25°C) | DMSO 3 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
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| ARM1
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| Actinonin
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities. |
| Amastatin hydrochloride
Amastatin hydrochloride is a slow, tight binding, competitive aminopeptidase (AP) inhibitor with Ki values of 0.26 nM, 30 nM, 52 nM for Aeromonas aminopeptidase, cytosolic leucine aminopeptidase, microsomal aminopeptidase. |
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