Bleomycin A5 hydrochloride  (Synonyms: Pingyangmycin hydrochloride)

Bleomycin A5 (Pingyangmycin) hydrochloride is a glycopeptide antibiotic with multiple biological activities, which can be isolated from Streptomyces. Bleomycin A5 hydrochloride exerts cytotoxic effects by binding to Fe²⁺ to form a complex, inducing single-strand and double-strand DNA breaks, and inhibiting DNA replication. Bleomycin A5 hydrochloride inhibits Drp1-mediated mitochondrial fission and suppresses PINK1/Parkin pathway-mediated mitophagy, ultimately triggering mitochondria-mediated cellular apoptosis. Bleomycin A5 hydrochloride can be used in cancer research^{[1][2][3][4][5]}.

Bleomycin A5 (25-400 μM; 6-72 h) hydrochloride induces mitochondria-mediated apoptosis in primary human nasal polyp-derived fibroblasts (NPDFs) in a time- and dose-dependent manner^[2].
Bleomycin A5 (200 μM; 48 h) hydrochloride inhibits Drp1-mediated mitochondrial fission in primary human nasal polyp-derived fibroblasts (NPDFs), leading to the formation of a fused, long tubular mitochondrial network^[2].
Bleomycin A5 (50-200 μM; 48 h) hydrochloride induces mitochondrial dysfunction in primary human nasal polyp-derived fibroblasts (NPDFs), and knockdown of Drp1 exacerbates this dysfunction, including increased superoxide accumulation, elevated mtDNA copy number, reduced ATP production, and aggravated mitochondrial membrane potential depletion^[2].
Bleomycin A5 (200 μM; 48 h) hydrochloride inhibits Drp1-mediated mitophagy in primary human nasal polyp-derived fibroblasts (NPDFs), and knockdown of Drp1 enhances this inhibitory effect, which is confirmed by the decreased levels of mitochondrial PINK1, Parkin, and LC3B^[2].
Bleomycin A5 hydrochloride is taken up by human cancer cells via mediation of the human transporter hCT2; specifically, the NT2/D1 testicular cancer cells with high hCT2 expression are 333 times more sensitive to it (IC₅₀ = 0.01 μM) than the HCT116 colon cancer cells with undetectable hCT2 expression (IC₅₀ = 3.33 μM)^[3].
Bleomycin A5 (10-160 μM; 48 h) hydrochloride induces concentration-dependent cytotoxicity in HCT116, HT29, H1299, A549, CHOK1, CHO745 and CHO3.1 cells, with the strongest activity observed in HCT116 cells (IC₅₀ = 9.9 μM) and reduced activity in GAG-deficient CHO745 cells (IC₅₀ = 327.7 μM)^[5].
Bleomycin A5 (10-80 μM; 4-48 h) hydrochloride significantly reduces the sulfation level of heparan sulfate in A549 and HCT116 cells (characterized by an increase in non-sulfated disaccharides and a decrease in sulfated disaccharides), and alters the disaccharide composition of chondroitin sulfate^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Hydrochloride of Bleomycin A5 (5 mg/kg; intratracheal administration; single dose) induces significant pulmonary inflammation and fibrosis in male Wistar rats, with inflammation peaking on day 7 and fibrosis progressing until day 28^[4].
Bleomycin A5 (1.2 mg/kg; intramuscular injection; once every 3 days; for 28 consecutive days) hydrochloride inhibits tumor growth of Lewis lung carcinoma and significantly reduces the sulfation levels of chondroitin sulfate (CS) and heparan sulfate (HS) in murine lung cancer^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1477.02

C₅₇H₉₀ClN₁₉O₂₁S₂

55658-47-4

[H]Cl.O=C(C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C)N[C@H](C(N[C@H](C)[C@@H](O)[C@H](C)C(N[C@]([C@H](O)C)([H])C(NCCC2=NC(C3=NC(C(NCCCNCCCCN)=O)=CS3)=CS2)=O)=O)=O)[C@H](C4=CN=CN4)O[C@H]5[C@H]([C@H]([C@H](O)[C@H](CO)O5)O)O[C@@]6([H])[C@H]([C@H]([C@H](O)[C@@H](CO)O6)OC(N)=O)O.[x]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Yang Y, et al. Bleomycin A5 sclerotherapy for cervicofacial lymphatic malformations. J Vasc Surg. 2011;53(1):150-155.  [Content Brief]

  [2]. Wu F, et al. Bleomycin A5 suppresses Drp1‑mediated mitochondrial fission and induces apoptosis in human nasal polyp‑derived fibroblasts. Int J Mol Med. 2021;47(1):346-360.  [Content Brief]

  [3]. Aouida M, et al. A new twist in cellular resistance to the anticancer drug bleomycin-A5. Curr Drug Metab. 2010;11(7):595-602.  [Content Brief]

  [4]. Pan JB, et al. Rolipram attenuates bleomycin A5-induced pulmonary fibrosis in rats. Respirology. 2009;14(7):975-982.  [Content Brief]

  [5]. Lan Y, et al. Pingyangmycin inhibits glycosaminoglycan sulphation in both cancer cells and tumour tissues. J Cell Mol Med. 2020;24(6):3419-3430.  [Content Brief]