Bestatin hydrochloride
Based on 12 publication(s) in Google Scholar
Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 65391-42-6
- Formula: C16H25ClN2O4
- Molecular Weight:344.83
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Publications Citing Use of MedChemExpress (MCE) Bestatin hydrochloride
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Cancer Res. 2025 Aug 29. [Abstract]
- Hemasphere. 2021 Jun 12;5(7):e602. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2025 Jun 23:101558. [Abstract]
- J Med Chem. 2023 Jun 22;66(12):7926-7942. [Abstract]
- Int J Oncol. 2019 Jul;55(1):331-339. [Abstract]
- J Med Chem. 2017 Mar 9;60(5):1817-1828. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2026 Oct;1872(7):168312. [Abstract]
- J Pharmacol Exp Ther. 2022 Aug;382(2):188-198. [Abstract]
- Toxicol Appl Pharmacol. 2025 May 4:500:117371. [Abstract]
- Discov Oncol. 2024 May 30;15(1):197. [Abstract]
- Dis Markers. 2022 Jan 11:2022:1839341. [Abstract]
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Biological Activity
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CD13 |
Bestatin enhances ATRA-induced differentiation and inhibits ATRA-driven phosphorylation of p38 MAPK in ATRA-sensitive APL NB4 cells. Bestatin can not reverse the differentiation block in ATRA-resistant APL MR2 cells. CD13 ligation with anti-CD13 antibody WM-15 results in phosphorylation of p38 MAPK, reduces the inhibition of Bestatin on the phosphorylation of p38 MAPK, and completely abolishes the enhancement of Bestatin on ATRA-inducing differentiation in NB4 cells[2]. Bestatin (600 μM)-treated cells progress slower through the cell cycle due to decreased rate of cell growth and the frequency of cell division. Bestatin inhibits the frequency of mitosis and the inherent multinuclearity in D. discoideum, and is not cytotoxic to D. discoideum cells at 0-600 μM. Bestatin inhibits aminopeptidase activity in lysates of PsaA-GFP- and GFP-expressing cells by 69.39% ± 10.5% and 39.93% ± 18.7% of control, respectively[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 65391-42-6
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Appearance Solid
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Molecular Weight 344.83
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Formula C16H25ClN2O4
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Color White to off-white
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SMILES
CC(C)C[C@@H](C(O)=O)NC([C@@H](O)[C@H](N)CC1=CC=CC=C1)=O.Cl
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Synonyms
Ubenimex hydrochloride
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Structure Classification
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Initial Source
Actinomycetes
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (12)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Cancer Res
tRF-21LeuTAA Promotes Oxidative Stress by Altering Glutathione Metabolic Enzymes to Support Prostate Cancer Progression. [Abstract]2025 Aug 29. PMID: 40882020
Bestatin hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Aug 29. [Abstract]
The LAP3 dipeptidase activity inhibitor Bestatin (200-400 μM; 48 h) significantly suppressed LAP3 and AKT enzyme activities and reduced p-mTORS2481 and pAKTS473 levels.
Bestatin hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Aug 29. [Abstract]
The LAP3 dipeptidase activity inhibitor Bestatin (200-400 μM; 48 h) induced a significant increase in intracellular GSH levels and a decrease in GSH degradation products Cys and Gly (resulting from Cys-Gly dipeptidase activity).
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Hemasphere
Novel Peptide-drug Conjugate Melflufen Efficiently Eradicates Bortezomib-resistant Multiple Myeloma Cells Including Tumor-initiating Myeloma Progenitor Cells. [Abstract]2021 Jun 12;5(7):e602. PMID: 34136753
Bestatin hydrochloride purchased from MedChemExpress. Usage Cited in: Hemasphere. 2021 Jun 12;5(7):e602. [Abstract]
Cytotoxicity of 125 and 250 nM melflufen in AMOaBTZ cells in the presence of BST (10 μM).
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Cell Mol Gastroenterol Hepatol
Exercise-induced Metabolite N-lactoyl-phenylalanine Ameliorates Colitis by Inhibiting M1 Macrophage Polarization Via the Suppression of the NF-κB Signaling Pathway. [Abstract]2025 Jun 23:101558. PMID: 40562095
Bestatin hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Mol Gastroenterol Hepatol. 2025 Jun 23:101558. [Abstract]
Western blot analysis of p65, p-p65, IκB-α, and p-IκB-α in RAW264.7 cells subjected to different treatment conditions. Bestatin (0.4 mM) significantly enhanced LPSinduced p65 phosphorylation, promoted IκB-α phosphorylation and degradation.
Bestatin hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Mol Gastroenterol Hepatol. 2025 Jun 23:101558. [Abstract]
Bestatin (50 mg/kg; i.p.; once daily) diminished the anti-inflammatory effects of high phenylalanine intake in mice.
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J Med Chem
2023 Jun 22;66(12):7926-7942. PMID: 37267712 -
Int J Oncol
Metformin induces TPC-1 cell apoptosis through endoplasmic reticulum stress-associated pathways in vitro and in vivo. [Abstract]2019 Jul;55(1):331-339. PMID: 31180536 -
J Med Chem
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. [Abstract]2017 Mar 9;60(5):1817-1828. PMID: 28218840 -
Biochim Biophys Acta Mol Basis Dis
CNDP2 drives renal tubular fibrosis in diabetic kidney disease via a sulfur-containing amino acids-mTOR signaling axis. [Abstract]2026 Oct;1872(7):168312. PMID: 42276307 -
J Pharmacol Exp Ther
Thymidine Kinase 1 Mediates the Synergistic Antitumor Activity of Ubenimex and Celecoxib via Regulation of Cell Cycle in Colorectal Cancer. [Abstract]2022 Aug;382(2):188-198. PMID: 35868865 -
Toxicol Appl Pharmacol
2025 May 4:500:117371. PMID: 40328338 -
Discov Oncol
Bestatin attenuates breast cancer stemness by targeting puromycin-sensitive aminopeptidase. [Abstract]2024 May 30;15(1):197. PMID: 38814491 -
Dis Markers
LTB4 Promotes Acute Lung Injury via Upregulating the PLC ε-1/TLR4/NF- κ B Pathway in One-Lung Ventilation. [Abstract]2022 Jan 11:2022:1839341. PMID: 35059042
Solvent & Solubility
DMSO : 100 mg/mL (290.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 20 mg/mL (58.00 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 10 mg/mL (29.00 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
Cells are harvested, washed, and lysed in NP-40 lysis buffer (50 mM Tris-HCl [pH 7.5], 150 mM NaCl, 0.5% NP-40). Total cell protein is quantified using the Bradford assay and 1-mg/mL protein aliquots are made. Ten microliters of total cell protein is mixed with 290 μL of substrate solution (0.1 mg/mL dithiothreitol [DTT], 0.1 mg/mL albumin, and 1 mM alanine-β-naphthylamide). Fluorometric measurements (340 nm excitation, 400 nm emission) are made after 15 and 30 min. The slope of the line between the 15- and 30-min measurements is used to represent aminopeptidase activity. Total cell protein is preincubated with bestatin, amastatin, puromycin, EDTA, and/or ZnCl2 for 20 min before the fluorometric aminopeptidase assay.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Growing cells (1×106 to 2×106 cells/mL) are diluted to 1.0×103 cells/mL and transferred (3 mL) into a well in a 12-well multiwell plate (2.5-cm diameter/well). Cells are treated with 0, 10, 50, 100, 300, or 600 μM Bestatin and allowed to grow at 21°C shaking at 180 rpm for 48 h. A hemocytometer is used to measure cell density after 0, 24, and 48 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Bestatin is dissolved in PBS. The agent (doses of 10, 1, and 0.1 mg/kg) is injected i.p. to non-cyclophosphamide-treated mice, 5 or 10 times at 24-h intervals before SRBC immunization. The mice are immunized 24 h after the last dose of bestatin. Pharmacological immunosuppression is induced by a single intraperitoneal injection of cyclophosphamide administered at a dose of 350 mg/kg, 12 days before SRBC immunization. Bestatin at the doses of 1 and 0.1 mg/kg is injected to cyclophosphamide-immunosuppressed mice i.p. five times at 48-h intervals or 10 times at 24-h intervals before SRBC immunization. The first dose of bestatin is administered 24 h after cyclophosphamide, while the last dose of the drug is injected 24h before SRBC immunization.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
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 [Content Brief]
[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. [Content Brief]
[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 [Content Brief]
[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 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.9000 mL | 14.4999 mL | 28.9998 mL | 72.4995 mL |
| 5 mM | 0.5800 mL | 2.9000 mL | 5.8000 mL | 14.4999 mL | |
| 10 mM | 0.2900 mL | 1.4500 mL | 2.9000 mL | 7.2499 mL | |
| 15 mM | 0.1933 mL | 0.9667 mL | 1.9333 mL | 4.8333 mL | |
| 20 mM | 0.1450 mL | 0.7250 mL | 1.4500 mL | 3.6250 mL | |
| 25 mM | 0.1160 mL | 0.5800 mL | 1.1600 mL | 2.9000 mL | |
| 30 mM | 0.0967 mL | 0.4833 mL | 0.9667 mL | 2.4166 mL | |
| 40 mM | 0.0725 mL | 0.3625 mL | 0.7250 mL | 1.8125 mL | |
| 50 mM | 0.0580 mL | 0.2900 mL | 0.5800 mL | 1.4500 mL | |
| DMSO | 60 mM | 0.0483 mL | 0.2417 mL | 0.4833 mL | 1.2083 mL |
| 80 mM | 0.0362 mL | 0.1812 mL | 0.3625 mL | 0.9062 mL | |
| 100 mM | 0.0290 mL | 0.1450 mL | 0.2900 mL | 0.7250 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Bestatin hydrochloride Related Classifications
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