Bleomycin Sulfate
Bleomycin Sulfate (BLENOXANE; CAS 9041-93-4) is a cytotoxic glycopeptide antibiotic mixture produced by Streptomyces verticillus strains and is classified as a chemotherapeutic agent. It chelates metal ions and activates oxygen molecules to generate reactive oxygen species, causing DNA single- and/or double-strand breaks.
Treatment with bleomycin sulfate inhibits DNA and protein synthesis, causing elongation of E. coli cells and enlargement of HeLa cells[ 1 ].
The drug is used in combination with doxorubicin and others to treat Hodgkin lymphoma, testicular cancer, and squamous cell carcinoma, and is administered by intralesional injection to treat plantar warts. For example, bleomycin sulfate shows moderate to marked activity against Rous sarcoma virus-induced mouse ascites sarcoma, particularly when F1 hybrid mice serve as host animals[ 2 ]. In addition, recent studies support the role of proinflammatory cytokines IL-18 and IL-1beta in bleomycin sulfate-induced lung injury in humans and mice[ 3 ].
Intratracheal or systemic administration of bleomycin induces pulmonary fibrosis in rodents and is commonly used to establish pulmonary fibrosis animal models, widely employed for anti-fibrotic drug evaluation.
References: 1.Suzuki H, Nagai K, Yamaki H, Tanaka N, Umezawa H. Mechanism of action of bleomycin. Studies with the growing culture of bacterial and tumor cells. J Antibiot (Tokyo) 1968,21:379-386.
[2]. Takeuchi M, Yamamoto T. Effects of bleomycin on transplantable mouse tumors. J Antibiot (Tokyo) 1968,21:631-637.
[3]. Hoshino T, Okamoto M, Sakazaki Y, Kato S, Young HA, Aizawa H. Role of proinflammatory cytokines IL-18 and IL-1beta in bleomycin-induced lung injury in humans and mice. Am J Respir Cell Mol Biol 2009,41:661-670.
- 1. Ruixuan Zhu, Yangfan Xiao, et al. "A novel LncRNA TUG1/miR-30d/e-3p/SNAI2 ceRNA axis drives dermal fibrosis in systemic sclerosis via direct transcriptional activation of COL1A1." Int Immunopharmacol. 2026 Aug 10:187:117232. PMID: 42574808
- 2. Zhang Jiashu, Liu Jingbao, et al. "Mitochondrial IRF3 drives pulmonary fibrosis by impairing mitophagy and triggering ferroptosis." Cell Signal. 2026 Apr 1:144:112517. PMID: 41932414
- 3. Yangeng Wang, Xie Liu, et al. "Inhalable Lipid Nanoparticles for Macrophage-Specific STING Gene Editing to Ameliorate Pulmonary Fibrosis." Mol Ther. 2026 Mar 6:S1525-0016(26)00188-7. PMID: 41795185
- 4. Yu-Qing Gu, Jing Wu, Tong Wang. "PINK1 deficiency alleviates bleomycin - induced pulmonary fibrosis in mice." Cell Signal. 2025 Sep:133:111868. PMID: 40373838
- 5. Yan Hu, Lulu Yang, et al. "m6A reader IGF2BP1 facilitates macrophage glycolytic metabolism and fibrotic phenotype by stabilizing THBS1 mRNA to promote pulmonary fibrosis." Cell Mol Life Sci. 2025 Apr 12;82(1):157. PMID: 40220148
- 6. Qi Lin, Yating Lin, et al. "ACSL1 improves pulmonary fibrosis by reducing mitochondrial damage and activating PINK1/Parkin mediated mitophagy." Sci Rep. 2024 Nov 3;14(1):26504. PMID: 39489819
- 7. Bingsi Tang, Jiangfan Yu, et al. "MiR-4769-3p suppresses adipogenesis in systemic sclerosis by negatively regulating the USP18/VDAC2 pathway." iScience. 2024 Jul 10;27(8):110483. PMID: 39156653
- 8. Bingsi Tang, Yaqian Shi, et al. "Silica's Silent Threat: Contributing to Skin Fibrosis in Systemic Sclerosis by Targeting the HDAC4/Smad2/3 Pathway." Environ Pollut. 2024 Aug 15:355:124194. PMID: 38782158
- 9. Ali H Shilleh, Scott Beard, et al. "Enrichment of stem cell-derived pancreatic beta-like cells and controlled graft size through pharmacological removal of proliferating cells." Stem Cell Reports. 2023 Jun 13;18(6):1284-1294. PMID: 37315522
- 10. Jingjing Zhang, Jinxin Qiu, et al. "Neuropilin-1 mediates lung tissue-specific control of ILC2 function in type 2 immunity." Nat Immunol. 2022 Feb;23(2):237-250. PMID: 35075279
- 11. Jiani Liu, Zixin Pi, et al. "Esomeprazole Alleviates Fibrosis in Systemic Sclerosis by Modulating AhR/Smad2/3 Signaling." Pharmacol Res. 2022 Feb;176:106057. PMID: 34995795
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| Physical Appearance | A solid |
| Storage | Store at -20° C |
| M.Wt | 1523 (average) |
| Cas No. | 9041-93-4 |
| Synonyms | Blenoxane;Bleo;Blexane; Bleomycin sulfate |
| Solubility | ≥125 mg/mL in DMSO with gentle warming; insoluble in EtOH; ≥151.3 mg/mL in H2O with ultrasonic |
| Chemical Name | Bleomycin sulfate |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
ADIPO-P2 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months. |
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Reaction Conditions |
2.5 μg/mL; 30 mins |
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Applications |
In ADIPO-P2 cells, Bleomycin Sulfate showed significant clastogenic effect, which even lasted for at least 10 days after exposure. |
| Animal experiment [2]: | |
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Animal models |
CD-1 mice |
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Dosage form |
5 mg/kg, 2 ml/kg, intratracheally |
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Applications |
Bleomycin Sulfate promoted the development of inflammation, resulting in severe pulmonary fibrosis, as well as simultaneous increasing of TGF-β1, Smad3 and STAT1. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Paviolo NS, Quiroga IY, Castrogiovanni DC, Bianchi MS, Bolzán AD. Telomere instability is present in the progeny of mammalian cells exposed to bleomycin. Mutat Res. 2012 Jun 1;734(1-2):5-11. [2]. Shi K, Jiang J, Ma T, Xie J, Duan L, Chen R, Song P, Yu Z, Liu C, Zhu Q, Zheng J. Dexamethasone attenuates bleomycin-induced lung fibrosis in mice through TGF-β, Smad3 and JAK-STAT pathway. Int J Clin Exp Med. 2014 Sep 15;7(9):2645-50. |
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| Description | Bleomycin Sulfate is a glycopeptide antibiotic and an anticancer agent for squamous cell carcinomas (SCC) with IC50 of 4 nM in UT-SCC-19A cells. | |||||
| Targets | UT-SCC-129 cells | |||||
| IC50 | 4 nM | |||||
Quality Control & MSDS
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