Description

Product Description

Bleomycin A5 Hydrochloride is a naturally derived glycopeptide antibiotic isolated from Streptomyces verticillus, exhibiting potent antitumor activity due to its ability to bind DNA and induce oxidative strand scission. As a member of the Bleomycin family, it has been extensively used in preclinical oncology studies targeting various tumor cell types, including squamous cell carcinoma, lymphomas, testicular carcinoma, and other rapidly proliferating malignant cells.

Bleomycin A5 Hydrochloride contains multiple functional groups that allow it to chelate metal ions, particularly Fe(II), facilitating the generation of reactive oxygen species (ROS). These ROS species catalyze oxidative cleavage of DNA, causing both single- and double-strand breaks. In vitro studies show that treatment with Bleomycin A5 Hydrochloride results in the accumulation of DNA damage markers such as γ-H2AX, activation of ATM/ATR pathways, and subsequent induction of cell cycle checkpoints, particularly G2/M arrest.

The compound has been applied in mechanistic research to elucidate cellular DNA repair pathways, including non-homologous end joining (NHEJ) and homologous recombination (HR). Researchers also use Bleomycin A5 Hydrochloride to investigate oxidative stress responses, mitochondrial integrity, and the interplay between DNA damage and apoptosis in tumor models. Its selective cytotoxicity toward rapidly dividing cells makes it a valuable tool for exploring tumor biology and chemotherapeutic mechanisms.

In combination studies, Bleomycin A5 Hydrochloride is used with platinum-based agents (e.g., cisplatin, carboplatin) and taxanes to evaluate additive or synergistic effects on DNA damage and apoptosis. These studies contribute to preclinical research aiming to improve chemotherapeutic efficacy, understand drug resistance mechanisms, and optimize dosing strategies.

Bleomycin A5 Hydrochloride’s aqueous solubility and stability in slightly acidic buffers allow for diverse experimental applications, including cell culture assays, flow cytometry analysis of apoptosis, Western blot evaluation of DNA damage markers, and preclinical in vivo tumor models. These properties make it suitable for mechanistic, pharmacodynamic, and combinatorial research in oncology.

In addition, Bleomycin A5 Hydrochloride is used in research exploring the generation of reactive oxygen species, free radical scavenging, and oxidative stress mitigation in cellular systems. Laboratory studies have shown that Bleomycin A5 Hydrochloride can cause selective cleavage of GC-rich DNA sequences, making it a precise tool for studying sequence-specific DNA damage responses.

Advanced research applications include using Bleomycin A5 Hydrochloride to investigate DNA damage checkpoint adaptation, senescence induction, and the interplay between apoptosis and autophagy in cancer cells. These studies provide insights into cellular mechanisms underlying chemotherapeutic response and contribute to drug development strategies.

The peptide component of Bleomycin A5 Hydrochloride also enables interactions with cell membranes, facilitating intracellular delivery and nuclear targeting. Preclinical studies often exploit these properties to evaluate intracellular ROS production, mitochondrial depolarization, and caspase-dependent apoptosis pathways.

Researchers have also applied Bleomycin A5 Hydrochloride in DNA repair inhibitor studies, using PARP inhibitors or ATM/ATR kinase inhibitors to study synergistic cytotoxic effects. These studies help delineate the contribution of specific repair pathways to tumor cell survival after DNA damage induction.

Further investigations employ Bleomycin A5 Hydrochloride to explore epigenetic regulation, including histone modifications and chromatin remodeling in response to DNA strand breaks. Such research expands understanding of the interplay between DNA damage, transcriptional regulation, and cell fate determination.

Bleomycin A5 Hydrochloride serves as an essential reagent for cancer biology, apoptosis research, and DNA damage studies, supporting a wide range of in vitro and in vivo preclinical models. Its multifaceted effects on DNA integrity, cell cycle, oxidative stress, and apoptosis make it a cornerstone compound for mechanistic oncology research.

Product Specifications

Mechanism of Action

Bleomycin A5 Hydrochloride functions primarily through DNA binding and oxidative cleavage. The glycopeptide binds DNA at specific sequences, chelates Fe(II) ions, and reacts with molecular oxygen to generate ROS. These reactive species cleave phosphodiester bonds, causing single- and double-strand breaks.

1. DNA Cleavage
   The Fe(II)-Bleomycin complex generates free radicals that attack DNA sugar-phosphate backbones, resulting in strand scission. Studies demonstrate preferential cleavage at GC-rich sequences, enabling sequence-specific DNA damage modeling.

2. Cell Cycle Arrest
   DNA breaks activate ATM/ATR kinases and downstream checkpoint proteins (Chk1/Chk2), causing G2/M phase arrest. This halts cell division, allowing the cell to attempt DNA repair or progress to apoptosis if damage is irreparable.

3. Apoptosis Induction
   Extensive DNA damage triggers intrinsic apoptotic pathways. Mitochondrial depolarization, cytochrome c release, and caspase-3 activation are observed in treated tumor cells. Upregulation of p53 and pro-apoptotic Bcl-2 family proteins contributes to cell death.

4. Oxidative Stress
   Bleomycin A5 Hydrochloride generates ROS in the nucleus and cytoplasm, amplifying DNA damage and modulating redox-sensitive signaling pathways. Researchers use this effect to study oxidative stress responses and antioxidant defense mechanisms.

5. Synergistic Cytotoxicity
   Combined with platinum agents or DNA repair inhibitors, Bleomycin A5 Hydrochloride enhances cell death in preclinical models. Studies explore combinatorial strategies for overcoming chemoresistance in tumor cells.

   

Side Effects (Research Context)

In vitro and in vivo studies reveal cytotoxicity consistent with DNA strand break induction. Cell viability depends on concentration, exposure duration, and cell type. Laboratory handling requires PPE, ventilated conditions, and adherence to biosafety protocols.

Bleomycin A5 Hydrochloride may induce oxidative stress, mitochondrial dysfunction, and apoptosis in normal and tumor cells. These effects are leveraged in research but highlight the need for careful dosing and controlled experimental conditions.

Potential research-related side effects include:

• DNA damage beyond intended targets

• Altered cell cycle progression

• Oxidative stress-related changes in cellular metabolism

• Dose-dependent cytotoxicity in normal cell lines

Researchers are advised to follow strict laboratory safety protocols. The compound is not approved for human, veterinary, or clinical use.

Keywords

Bleomycin A5 Hydrochloride, glycopeptide antibiotic, DNA damage, apoptosis research, cell cycle arrest, chemotherapeutic research chemical, cancer research, high purity compound, laboratory study, preclinical oncology

Shipping Guarantee

All shipments are handled using validated cold-chain logistics to preserve compound integrity. Each package is sealed in moisture-proof containers with secondary protective wrapping and continuous temperature monitoring. Products are shipped via express international couriers with full tracking and insurance coverage.

Trade Assurance

We ensure product authenticity, verified ≥99% purity, and compliance with analytical standards (HPLC, MS, and NMR). Each batch is supplied with a Certificate of Analysis (CoA). Our trade assurance policy guarantees replacement or refund for any deviation from listed specifications.

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Disclaimer

All products listed are intended for laboratory research use only and not for human or veterinary use. They are not drugs, medical devices, or diagnostics and should not be administered to humans or animals. Researchers must handle all materials in accordance with institutional biosafety and chemical safety guidelines. The information provided is for scientific reference only and does not imply therapeutic efficacy, safety, or regulatory approval.