Bestatin (Synonyms: NK 421, NSC 265489) |
| カタログ番号GC11780 |
アミノペプチダーゼ阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 58970-76-6
Sample solution is provided at 25 µL, 10mM.
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Bestatin is known to be an inhibitor of Aminopeptidase N (APN/CD13), which has the IC50 values of 14.9±3.4μM[1]. Bestatin can also inhibits aminopeptidase B and LTA4 hydrolase[2, 3]. Bestatin was shown to enhance antibody-dependent cell mediated cytotoxicity and natural killer cell activity[4].
Bestatin (10μM; 24h) significantly reduced melflufen (125 or 250nM; 24h) induced cytotoxicity in AMOaBTZ cells[5]. Bestatin (0.25mM; 24h) can inhibit the migration and proliferation of breast cancer cells[6].
Bestatin (30mg/kg; i.p. ; 15min) alleviated the acute lung injury in one-lung ventilation model rats[7]. Bestatin (0.1 or 1 or 10mg/kg; i.p. ; 5 or 10 times at 24h intervals) potentiated the humoral response to sheep erythrocytes (SRBC; i.p. ) suspension in mice, resulting in an increased number of plaque-forming cells[8].
References:
[1] LUAN Y, MA C, SUI Z, et al. LYP3, a new bestatin derivative for aminopeptidase N inhibition [J]. Med Chem, 2011, 7(1): 32-6.
[2] JIA M R, WEI T, XU W F. The Analgesic Activity of Bestatin as a Potent APN Inhibitor [J]. Front Neurosci, 2010, 4(50.
[3] AOZUKA Y, KOIZUMI K, SAITOH Y, et al. Anti-tumor angiogenesis effect of aminopeptidase inhibitor bestatin against B16-BL6 melanoma cells orthotopically implanted into syngeneic mice [J]. Cancer Lett, 2004, 216(1): 35-42.
[4] SCORNIK O A, BOTBOL V. Bestatin as an experimental tool in mammals [J]. Current drug metabolism, 2001, 2(1): 67-85.
[5] BYRGAZOV K, BESSE A, KRAUS M, et al. Novel Peptide-drug Conjugate Melflufen Efficiently Eradicates Bortezomib-resistant Multiple Myeloma Cells Including Tumor-initiating Myeloma Progenitor Cells [J]. Hemasphere, 2021, 5(7): e602.
[6] MA Y, YANG X, PAN P, et al. Bestatin attenuates breast cancer stemness by targeting puromycin-sensitive aminopeptidase [J]. Discov Oncol, 2024, 15(1): 197.
[7] LUO J, MA Q, TANG H, et al. LTB4 Promotes Acute Lung Injury via Upregulating the PLCepsilon-1/TLR4/NF-kappaB Pathway in One-Lung Ventilation [J]. Dis Markers, 2022, 2022(1839341.
[8] LIS M, SZCZYPKA M, SUSZKO A, et al. The effects of bestatin on humoral response to sheep erythrocytes in non-treated and cyclophosphamide-immunocompromised mice [J]. Immunopharmacol Immunotoxicol, 2013, 35(1): 133-8.
| Cell experiment [1]: | |
Cell lines | Mammary breast cancer cell lines SKRB3 |
Preparation Method | SKRB3 were cultured in McCoy’s 5A supplemented with 10% fetal bovine serum at 37°C in a humidified 5% CO2 atmosphere. Cells were cultured until they were 70% confluent in 6‑well plate, then a wound was drawn by a sterile 200μl pipette tip. Subsequently, cells were cultured in fresh serum-free medium with/without 0.25mM Bestatin for 24h. |
Reaction Conditions | 0.25mM; 24h |
Applications | Bestatin can inhibit the migration and proliferation of breast cancer cells. |
| Animal experiment [2]: | |
Animal models | male and female Balb/c mice |
Preparation Method | The mice were immunized intraperitoneally with 0.2ml of 10% SRBC suspension (4×108 cells per mouse). The blood was taken from the jugular vein of cross-bred clinically healthy sheep. The sheep blood was collected in sterile manner into Alsever’s solution containing glucose (2.05%), sodium citrate (0.8%), sodium chloride (0.42%), and citric acid (0.055%) and kept there at 4℃ for at least 3 days. The SRBC suspension was prepared extempore in phosphate-buffered saline (PBS). Bestatin was dissolved in PBS. The agent (doses of 10, 1, and 0.1mg/kg) was injected i.p. to mice, 5 or 10 times at 24h intervals before SRBC immunization. The mice were immunized 24h after the last dose of bestatin. |
Dosage form | 0.1 or 1 or 10mg/kg; i.p. ; 5 or 10 times at 24h intervals |
Applications | Bestatin potentiated the humoral response to sheep erythrocytes in mice, resulting in an increased number of plaque-forming cells and 2-mercaptoethanol-resistant anti-SRBC hemagglutinations. |
References: | |
| Cas No. | 58970-76-6 | SDF | |
| 同義語 | NK 421, NSC 265489 | ||
| Chemical Name | (2S)-2-[[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]amino]-4-methylpentanoic acid | ||
| Canonical SMILES | CC(C)CC(C(=O)O)NC(=O)C(C(CC1=CC=CC=C1)N)O | ||
| Formula | C16H24N2O4 | M.Wt | 308.37 |
| 溶解度 | ≥ 12.34mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2429 mL | 16.2143 mL | 32.4286 mL |
| 5 mM | 0.6486 mL | 3.2429 mL | 6.4857 mL |
| 10 mM | 0.3243 mL | 1.6214 mL | 3.2429 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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