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| 50mg |
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| 250mg |
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Ubenimex HCl (Bestatin hydrochloride) is a novel and potent CD13 inhibitor or Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor with the potential to be used for cancer treatment.
| ln Vitro |
In ATRA-sensitive APL NB4 cells, bestatin promotes ATRA-induced differentiation and prevents ATRA-driven p38 MAPK phosphorylation. The differentiation block in ATRA-resistant APL MR2 cells is not reversed by bestatin. When CD13 is bound to the anti-CD13 antibody WM-15, p38 MAPK is phosphorylated, Bestatin's inhibitory effect on p38 MAPK phosphorylation is lessened, and Bestatin's improvement of ATRA-induced NB4 cell differentiation is totally eliminated [2]. Cells treated with bestatin (600 μM) underwent slower cell cycle progression because their frequency of cell division and growth were decreased. Between 0-600 μM, bestatin does not cause cytotoxicity to D. discoideum cells, but it does suppress the frequency of mitosis and intrinsic multinucleation in these cells. In PsaA-GFP and GFP-expressing cell lysates, bestatin reduced aminopeptidase activity by 69.39% ± 10.5% and 39.93% ± 18.7% of the control, respectively [4].
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| ln Vivo |
When compared to diabetic vehicle-treated mice, bestatin (20 μM) dramatically inhibited MMP-9-specific gel resolution band density and considerably lowered CD13 expression in diabetic mice. In diabetic mice, treatment with betatin markedly reduced the expression of heparanase and VEGF. In the retina of diabetic mice, intravitreal betatin therapy markedly reduced the expression of VEGF and HIF-1α. Moreover, the administration of intravitreal betatin markedly suppressed the elevated expression of heparanase in the retina of mice with diabetes [1]. Prior to augmenting the humoral response to SRBC antigens, treatment with Bestatin (10, 1, and 0.1 mg/kg, i.p.) produced hemolytic anti-SRBC antibodies (PFC) in the spleen and 2-ME resistant serum hemagglutinin titers. a rise in cell count (dose: 0.1 mg/kg). After cyclophosphamide injection, mice were given bestatin (1 and 0.1 mg/kg) five times the following day. This did not alter the drug's inhibitory effect on PFC numbers and, in fact, caused a further decrease in total anti-SRBC hemagglutinin at the antigen stimulation level. On the seventh day, it is 1 mg/kg [3].
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| References |
[1]. Hossain A, et al. Protective effects of bestatin in the retina of streptozotocin-induced diabetic mice. Exp Eye Res. 2016 Aug;149:100-6
[2]. Qian X, 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. 2016 May-Jun;23(3):e680-9. [3]. Lis M, et al. The effects of bestatin on humoral response to sheep erythrocytes in non-treated and cyclophosphamide-immunocompromised mice. Immunopharmacol Immunotoxicol. 2013 Feb;35(1):133-8 [4]. Poloz Y, et al. Bestatin inhibits cell growth, cell division, and spore cell differentiation in Dictyostelium discoideum. Eukaryot Cell. 2012 Apr;11(4):545-57 |
| Molecular Formula |
C16H25CLN2O4
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|---|---|
| Molecular Weight |
344.8337
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| CAS # |
65391-42-6
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| Related CAS # |
Bestatin;58970-76-6;Bestatin-d7 hydrochloride;Bestatin trifluoroacetate;223763-80-2
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| SMILES |
Cl[H].O([H])[C@]([H])(C(N([H])[C@]([H])(C(=O)O[H])C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)[C@@]([H])(C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])N([H])[H]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~724.99 mM)
H2O : ~100 mg/mL (~290.00 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (145.00 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9000 mL | 14.4999 mL | 28.9998 mL | |
| 5 mM | 0.5800 mL | 2.9000 mL | 5.8000 mL | |
| 10 mM | 0.2900 mL | 1.4500 mL | 2.9000 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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