Description

Product Description

Ubenimex (bestatin), CAS 58970-76-6, is a potent and selective inhibitor of aminopeptidases such as leukotriene A4 hydrolase (LTA4H) and aminopeptidase N (CD13). These enzymes play critical roles in immune cell regulation, antigen processing, angiogenesis, and tumor proliferation. Ubenimex has been widely used in preclinical studies to investigate its dual functions: enhancing immune-mediated tumor suppression and directly inhibiting tumor cell proliferation.

As a lyophilized powder, Ubenimex provides excellent stability and precise dosing, allowing researchers to formulate solutions for in vitro and in vivo studies. Its high purity ensures consistent experimental reproducibility in studies of immune modulation, apoptosis, and cytotoxicity.

Chemical and Structural Features

Ubenimex is a small molecule with the molecular formula C14H26N2O3 and a molecular weight of 258.36 g/mol. Structurally, it is a dipeptide analog that mimics natural substrates of aminopeptidases, binding to their active sites and inhibiting enzymatic activity. This selective inhibition affects both immune and cancer cells, making it a valuable preclinical tool for studying tumor immunity and pharmacological modulation of aminopeptidases.

Pharmacological Significance

Ubenimex exerts multifaceted effects in preclinical models:

• Immune Modulation: Enhances cytotoxic T-cell and natural killer (NK) cell activity by inhibiting CD13 and other immunosuppressive aminopeptidases.

• Tumor Growth Inhibition: Suppresses proliferation in various tumor cell lines via aminopeptidase blockade and apoptotic pathway activation.

• Apoptosis Induction: Triggers intrinsic and extrinsic apoptotic pathways in cancer cells, including caspase activation and mitochondrial depolarization.

• Microenvironment Regulation: Modulates tumor angiogenesis, extracellular matrix remodeling, and immune cell infiltration.

Ubenimex is particularly suitable for studies in hematologic malignancies, solid tumors, and models of tumor immunotherapy, providing a dual mechanism to investigate both immune enhancement and direct tumor suppression.

Preclinical Applications

• Immune Response Studies: Analyze T-cell, NK-cell activity, and dendritic cell function in vitro and in vivo.

• Cancer Research: Evaluate cytotoxicity, apoptosis, and tumor growth suppression in preclinical models.

• Combination Therapy Research: Study synergistic or antagonistic effects with chemotherapeutics, checkpoint inhibitors, or kinase inhibitors.

• Mechanism of Resistance Studies: Explore resistance mechanisms via aminopeptidase expression changes or immune escape pathways.

• Pharmacodynamic and Pharmacokinetic Evaluations: Lyophilized powder allows precise reconstitution for dosing in animal models.

  

Product Specifications

Mechanism of Action

Aminopeptidase Inhibition

Ubenimex selectively binds to active sites of aminopeptidases, preventing peptide substrate cleavage. Key effects include:

• CD13 (Aminopeptidase N) Inhibition: Reduces tumor cell invasion, angiogenesis, and proliferation.

• LTA4H Inhibition: Modulates leukotriene metabolism and inflammatory responses in immune cells.

Immune Enhancement

• Enhances T-cell cytotoxicity and NK-cell activity

• Modulates antigen presentation and cytokine release

• Reduces immunosuppressive signaling within the tumor microenvironment

Apoptosis Induction

• Mitochondrial depolarization and cytochrome c release

• Caspase-3 and caspase-9 activation

• ROS generation contributing to cytotoxic stress

• G1/S cell-cycle arrest in tumor cells

Preclinical Research Applications

• Mechanistic studies in immune-oncology models

• Combination therapy with chemotherapeutics or immunomodulators

• Resistance mechanism exploration in cancer and immune cells

  

Ubenimex Side Effects (Preclinical Observations)

Cellular Effects

• Reduced proliferation in tumor cells

• G1/S phase cell-cycle arrest

• ROS-mediated cytotoxic stress

• Modulation of immune cell activity

Apoptotic Effects

• Activation of intrinsic apoptosis pathways via caspase cascade

• Mitochondrial depolarization and cytochrome c release

• p53-dependent and independent cell death

Laboratory Handling

• Use appropriate PPE and fume hood

• Store at 2–8 °C, protected from light and moisture

• Avoid repeated freeze-thaw cycles

Handle strictly as cytotoxic research reagent

Keywords

Ubenimex, Bestatin, aminopeptidase inhibitor, CD13 inhibitor, LTA4H inhibitor, immune modulation research, apoptosis studies, tumor cytotoxicity, preclinical immunology, cancer microenvironment research, combination therapy studies, high-purity research chemical, factory small-molecule supplier, China chemical manufacturer, OEM & bulk production, laboratory research reagent

Shipping Guarantee

All Ubenimex shipments of Ubenimex lyophilized powder are handled using validated cold-chain logistics to maintain compound stability. Packages are sealed with protective wrapping and shipped via express international couriers with tracking and insurance. Conditions are monitored to preserve the integrity of the powder during transit.

Trade Assurance

We guarantee the authenticity and quality of all Ubenimex batches. Purity is verified at ≥99% via HPLC, MS, and NMR. Certificates of Analysis (CoA) are provided for each batch. Replacement or refund is assured for any deviation from listed specifications.

Payment Support

Flexible global payment options include:

• PayPal

• Major credit cards (Visa, MasterCard, American Express)

• Bank transfer (T/T)

• Cryptocurrencies (USDT, Bitcoin, Ethereum)

All Ubenimex transactions are encrypted to ensure security and confidentiality.

Disclaimer

Ubenimex is supplied strictly for laboratory research purposes. Not for human or veterinary use. Researchers must follow institutional safety and chemical handling protocols. Supplier assumes no liability for misuse.

References

• PubChem: Ubenimex (CID 6977917)

• ChEMBL: Ubenimex Bioactivity Summary (CHEMBL1201613)

• DrugBank: Ubenimex – DB04983

• PubMed: Bestatin (Ubenimex) Mechanism Studies (PMID 15598748)

• IUPHAR/BPS Guide to Pharmacology: Aminopeptidase Inhibitors