A8331-10mg | Bleomycin Sulfate [9041-93-4] Clinisciences

Bleomycin sulfate (BLENOXANE®) is a mixture of cytotoxic glycopeptide antibiotics produced by a strain of streptomyces verticillus. This component is known to cause single and/ or double-stranded breaks in DNA through approximating metals and coordinate dioxygen to generate the active species.

Bleomycin sulfate treatment resulted in elongation of E. coli cells and enlargement of HeLa cells through inhibiting DNA and protein syntheses [1].

This component is widely used in the treatment of Hodgkin's lymphoma in combination with doxorubicin, testicular cancer, squamous cell carcinomas, pulmonary fiborosis as well as in the treatment of plantar warts. For instance, Bleomycin sulfate was also shown to have

moderate to marked effects upon Rous sarcoma virus induced mouse ascites sarcoma, particularly when F1 hybrid mice were employed as host animals [2]. In addition, recent studies support the role of the proinflammatory cytokines IL-18 and IL-1beta in the mechanism of bleomycin sulfate –induced human and mouse lung injury [3].

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. 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
2. 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
3. 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
4. Zhao K, Wang X, et al. "A long noncoding RNA sensitizes genotoxic treatment by attenuating ATM activation and homologous recombination repair in cancers." PLoS Biol. 2020;18(3):e3000666. PMID: 32203529
5. Thompson PJ, Shah A, et al. "Targeted Elimination of Senescent Beta Cells Prevents Type 1 Diabetes." Cell Metab. 2019 Feb 14. pii: S1550-4131(19)30021-X. PMID: 30799288

Physical Appearance	A solid
Storage	Store at -20° C
M.Wt	1512.6
Cas No.	9041-93-4
Formula	C₅₅H₈₅N₁₇O₂₅S₄
Synonyms	Blenoxane;Bleo;Blexane
Solubility	≥125 mg/mL in DMSO with gentle warming; insoluble in EtOH; ≥151.3 mg/mL in H2O with ultrasonic
Chemical Name	3-[[2-[2-[2-[[(2R,3R)-2-[[(2R,3R,4S)-4-[[(2S)-2-[[6-amino-2-[(1S)-3-amino-1-[[(2R)-2,3-diamino-3-oxopropyl]amino]-3-oxopropyl]-5-methylpyrimidine-4-carbonyl]amino]-3-[(2S,3R,4R,5R,6R)-3-[(2R,3S,4S,5R,6R)-4-carbamoyloxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-
SDF	Download SDF
Canonical SMILES	CC1=C(N=C(N=C1N)C(CC(=O)N)NCC(C(=O)N)N)C(=O)NC(C(C2=CN=CN2)OC3C(C(C(C(O3)CO)O)O)OC4C(C(C(C(O4)CO)O)OC4C(C(C(C(O4)CO)O)OC(=O)N)O)C(=O)NC(C)C(C(C)C(=O)NC(C(C)O)C(=O)NCCC5=NC(=CS5)C6=NC(=CS6)C(=O)NCCC[S+](C)C)O.OS(=O)(=O)[O-]
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]:
Cell lines	ADIPO-P2 cells
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.
Reaction Conditions	2.5 μg/mL; 30 mins
Applications	In ADIPO-P2 cells, Bleomycin Sulfate showed significant clastogenic effect, which even lasted for at least 10 days after exposure.
Animal experiment [2]:
Animal models	CD-1 mice
Dosage form	5 mg/kg, 2 ml/kg, intratracheally
Applications	Bleomycin Sulfate promoted the development of inflammation, resulting in severe pulmonary fibrosis, as well as simultaneous increasing of TGF-β1, Smad3 and STAT1.
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.
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.

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