Cat. No.: HY-B0134B

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Bestatin trifluoroacetate

Name: Bestatin trifluoroacetate
Brand: MedChemExpress
SKU: HY-B0134B
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(Synonyms: Ubenimex trifluoroacetate)

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

Bestatin trifluoroacetate 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.

CAS No.: 223763-80-2
Formula: C₁₈H₂₅F₃N₂O₆
Molecular Weight:422.40

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

Bestatin trifluoroacetate Chemical Structure

CAS No.: 223763-80-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Bestatin trifluoroacetate is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.

IC₅₀ & Target

^[1]^[2]^[3]^[4]

CD13

All Aminopeptidase Isoforms :

CD13
LTA4H

All Antibiotic Isoforms :

In Vitro

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. .

In Vivo

Bestatin (20 μM) significantly reduces CD13 expression in diabetic mice and results a significant inhibition of MMP-9 specific gelationolytic band densities compared to diabetic vehicle-treated mice. Bestatin treatment significantly inhibits the expression of VEGF and heparanase in diabetic mice. Intravitreal bestatin treatment significantly downregulates the expression of both HIF-1α and VEGF in diabetic mice retinas. Furthermore, the upregulated expression of heparanase in diabetic mice retinas is significantly inhibited by intravitreal bestatin treatment^[1]. Bestatin (10, 1, and 0.1mg/kg, i.p.) treatment before the antigen-potentiated humoral response to SRBC results in an increased number of splenocytes producing hemolytic anti-SRBC antibodies (PFC) and the 2-ME-resistant serum hemagglutinin titer (at a dose of 0.1 mg/kg). Bestatin (1 and 0.1 mg/kg) administered to mice five times on alternate days after cyclophosphamide injection does not change the suppressive effect of the drug regarding the number of PFC, and even causes the further decrease of the total anti-SRBC hemagglutinins at dose of 1 mg/kg on day 7 after antigen stimulation^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 223763-80-2
Molecular Weight 422.40
Formula C₁₈H₂₅F₃N₂O₆
SMILES

FC(F)(C(O)=O)F.CC(C)C[C@@H](C(O)=O)NC([C@@H](O)[C@H](N)CC1=CC=CC=C1)=O
Synonyms

Ubenimex trifluoroacetate
Structure Classification
- Ketones, Aldehydes, Acids
Initial Source
- Microorganisms
Streptomyces olivoreticuli
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (13)

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Journal Impact Factor

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 trifluoroacetate 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-mTOR^S2481 and pAKT^S473 levels.

Bestatin trifluoroacetate 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).
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 trifluoroacetate 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).
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;19(10):101558. PMID: 40562095

Bestatin trifluoroacetate purchased from MedChemExpress. Usage Cited in: Cell Mol Gastroenterol Hepatol. 2025;19(10):101558. [Abstract]

Western blot analysis of p65, p-p65, I_κB-_α, and p-I_κB-_α in RAW264.7 cells subjected to different treatment conditions. Bestatin (0.4 mM) significantly enhanced LPSinduced p65 phosphorylation, promoted I_κB-_α phosphorylation and degradation.

Bestatin trifluoroacetate purchased from MedChemExpress. Usage Cited in: Cell Mol Gastroenterol Hepatol. 2025;19(10):101558. [Abstract]

Bestatin (50 mg/kg; i.p.; once daily) diminished the anti-inflammatory effects of high phenylalanine intake in mice.
J Med Chem

Discovery of Small-Molecule Degraders for Alpha-Synuclein Aggregates. [Abstract]

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

OAT1/3 regulate the absorption of CP-25 in the rat synovium. [Abstract]

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
Vita

2026 Apr 7.
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Keywords

Bestatin trifluoroacetate

13 Cited Publications

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Bestatin trifluoroacetate

Publications Citing Use of MedChemExpress (MCE) Bestatin trifluoroacetate

All Aminopeptidase Isoforms

All Antibiotic Isoforms