Antitumor antibiotic
- Antibiotic with anti-cancer and apoptotic properties
- Radiomimetic DNA-cleaving agent that produces double and single DNA strand breaks through an oxygen-radical-dependent mechanism
- Highly cited
Bleomycin consists in a complex of 11 glycopeptide anti-cancer antibiotics originally isolated from Streptomyces verticillus. The dominant components of the complex are bleomycin A2 and B2, which typically represent >90% of the total weight. Bleomycin has found clinical application in the treatment of a range of tumors. Bleomycin acts by intercalation of DNA and RNA. In the presence of oxygen and metal ions (e.g. copper and iron), Bleomycin forms a pseudo-enzyme that induces DNA cleavage.
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Product Details
| Alternative Name |
Blenoxane |
|---|---|
| Appearance |
White crystalline solid. |
| CAS |
9041-93-4 |
| Formula |
C55H85N17O21S3 (For A2) |
| MI |
14: 1318 |
| MW |
1415.6 (For A2) |
| Purity |
≥98% (HPLC) |
| RTECS |
EC5991990 |
| Solubility |
Soluble in 100% methanol or water (20mg/ml). |
| Source |
Isolated from Streptomyces sp. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored, as supplied, at -20°C. Stock solutions are stable for up to 3 months at -20°C. |
|---|---|
| Long Term Storage |
-20°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- Deregulated immune cell recruitment orchestrated by c-MET impairs pulmonary inflammation and fibrosis: Barbosa-Matos, C., Borges-Pereira, C., et al.; Respir. Res. 25, 257 (2024), Abstract
- Interstitial Macrophages Lead Early Stages of Bleomycin-Induced Lung Fibrosis and Induce Fibroblasts Activation: Libório-Ramos, S., Barbosa-Matos, C., et al.; Cells 12, (2023), Abstract
- Skin fibrosis and recovery is dependent on Wnt activation via DPP4: A. Jussila, et al.; J. Invest. Dermatol. 142, 1597 (2022), Abstract
- Inhibiting a mRNA motif binding protein that mediates TGF-β1 upregulation of translation attenuates pulmonary fibrosis in mice: Chen, W., Pilling, D., et al.; bioRxiv , (2022)
- A Proximity Ligation Method to Detect Proteins Bound to Single-Stranded DNA after DNA End Resection at DNA Double-Strand Breaks: F.C. Fowler & J.K. Tyler; Methods Protoc. 5, 3 (2022), Abstract
- Ameliorating Fibrosis in Murine and Human Tissues with END55, an Endostatin-Derived Fusion Protein Made in Plants: L. Mlakar, et al.; Biomedicines 10, 2861 (2022), Abstract
- A model of the aged lung epithelium in idiopathic pulmonary fibrosis: H. Shaghaghi, et al.; Aging 13, 16922 (2021), Abstract — Full Text
- Discovery of the S1P2 antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a preclinical candidate for the treatment of idiopathic pulmonary fibrosis: O. Mammoliti, et al.; J. Med. Chem. 64, 6037 (2021), Abstract
- Adipocyte lipolysis abrogates skin fibrosis in a Wnt/DPP4-dependent manner: Jussila, A., Caves, E., et al.; bioRxiv , (2021)
- Impaired HSF1 transactivation drives proteostasis collapse and senescent phenotype of IPF lung fibroblast: Cuevas-Mora, K., Roque, W., et al.; bioRxiv , (2020)
- Transcriptomics, metabolomics and lipidomics of chronically injured alveolar epithelial cells reveals similar features of IPF lung epithelium: Roque, W., Cuevas-Mora, K., et al.; bioRxiv , (2020)
- Thymic stromal lymphopoietin protects in a model of airway damage and inflammation via regulation of caspase-1 activity and apoptosis inhibition: N. Shubin, et al.; Mucosal Immunol. 13, 584 (2020), Abstract — Full Text
- Inflammatory drivers of cardiovascular disease: molecular characterization of senescent coronary vascular smooth muscle cells: S. Stojanovic, et al.; Front. Physiol. 11, 520 (2020), Abstract — Full Text
- Electrochemotherapy in 3D ocular melanoma spheroids using a customized electrode: M. Fiorentzis, et al.; J. Vis. Exp. 158, e60611 (2020), Abstract
- Direct intrabronchial administration to improve the selective agent deposition within the mouse lung: S. Liao, et al.; J. Vis. Exp. 147, e59450 (2019), Abstract
- MERIT40-dependent recruitment of tankyrase to damaged DNA and its implication for cell sensitivity to DNA-damaging anticancer drugs: O. Keiji et al.; Oncotarget 9, 25844 (2018), Abstract — Full Text
- The hypoxic tumor microenvironment in vivo selects tumor cells with increased survival against genotoxic stresses: Kim, H., Lin, Q., et al.; Cancer Lett. 431, 142 (2018), Abstract
- ASF1a Promotes Non-homologous End Joining Repair by Facilitating Phosphorylation of MDC1 by ATM at Double-Strand Breaks.: K.Y Lee et al.; Mol. Cell 5, 51 (2017), Abstract — Full Text
- Overexpression screens identify conserved dosage chromosome instability genes in yeast and human cancer: S. Duffy, et al.; PNAS 113, 9967 (2016), Application(s): Sensitivity to Genotoxic Agents, Yeast strains carrying each dCIN candidate , Abstract — Full Text
- Adaptation of HepG2 cells to a steady-state reduction in the content of protein phosphatase 6 (PP6) catalytic subunit: Boylan, J. M., Salomon, A. R., et al.; Exp. Cell Res. 335, 224 (2015), Abstract
- Extracellular ATP mediates the late phase of neutrophil recruitment to the lung in murine models of acute lung injury: D. Shah, et al.; Am. J. Physiol. Lung Cell. Mol. Physiol. 306, L152 (2014), Abstract — Full Text
- Common variants of Drosophila melanogaster Cyp6d2 cause camptothecin sensitivity and synergize with loss of Brca2: Thomas, A. M., Hui, C., et al.; G3 (Bethesda) 3, 91 (2013), Abstract
- Targeting Her-2+ breast cancer cells with bleomycin immunoliposomes linked to LLO: M. Kullberg, et al.; Mol. Pharm. 9, 2000 (2012), Abstract
- Twist1-mediated adriamycin-induced epithelial-mesenchymal transition relates to multidrug resistance and invasive potential in breast cancer cells: Li, Q. Q., Xu, J. D., et al.; Clin. Cancer Res. 15, 2657 (2009), Abstract
- Involvement of CD147 in regulation of multidrug resistance to P-gp substrate drugs and in vitro invasion in breast cancer cells: Li, Q. Q., Wang, W. J., et al.; Cancer Sci. 98, 1064 (2007), Abstract
- Bleomycin-induced alterations in DNA replication: relationship to DNA damage: J. Dziegielewski, et al.; Biochemistry 40, 704 (2001), Abstract
- Bleomycin: new perspectives on the mechanism of action: S.M. Hecht; J. Nat. Prod. 63, 158 (2000), Abstract
- Synergistic effects of laserthermia and bleomycinsulfate on micronuclei formation in cytokinesis-blocked HeLa cells: A.S. Monfared & H. Mozdarani; Irn. J. Med. Sci. 24, 87 (1999)
- Changes in c-Jun but not Bcl-2 family proteins in p53-dependent apoptosis of mouse cerebellar granule neurons induced by DNA damaging agent bleomycin: T. Araki, et al.; Brain Res. 794, 239 (1998), Abstract
- Regulation of apoptosis in mouse hepatocytes and alteration of apoptosis by nongenotoxic carcinogens: J.G. Christensen, et al.; Cell Growth Differ. 9, 815 (1998), Abstract
- p53 activates the CD95 (APO-1/Fas) gene in response to DNA damage by anticancer drugs: M. Muller, et al.; J. Exp. Med. 188, 2033 (1998), Abstract
- Sequence-specific changes in the metal site of ferric bleomycin induced by the binding of DNA: J.W. Sam, et al.; J. Biol. Chem. 273, 16090 (1998), Abstract
- Antiangiogenic chemotherapeutic agents: characterization in comparison to their tumor growth inhibition in human renal cell carcinoma models: M. Schirner, et al.; Clin. Cancer Res. 4, 1331 (1998), Abstract
- Induction of apoptosis by bleomycin in resting and cycling human lymphocytes: P. Vernole, et al.; Mutagenesis 13, 209 (1998), Abstract
- Cleavage of tRNA by Fe(II)-bleomycin: A. Huttenhofer, et al.; J. Biol. Chem. 267, 24471 (1992), Abstract
- Chromatin structure during bleomycin-induced DNA damage and repair: B.P. Cuiffo, et al.; J. Free Radic. Biol. Med. 1, 139 (1985), Abstract
- Specificity of deoxyribonucleic acid cleavage by bleomycin, phleomycin, and tallysomycin: J. Kross, et al.; Biochemistry 21, 4310 (1982), Abstract
- Bleomycin and other antitumor antibiotics of high molecular weight: H. Umezawa; Antimicrob. Agents Chemother. (Bethesda) 5, 1079 (1965), Abstract
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Last modified: May 29, 2024
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