Suramin hexasodium salt
Suramin hexasodium salt, as a polysulfonated naphthylurea, is a potent competitive inhibitor of DNA topoisomerase II, with an IC50 of 5 μM.
DNA topoisomerase II cuts both strands of the DNA helix simultaneously to manage DNA tangles and supercoils. Once cut, the ends of the DNA are separated and another DNA duplex passed through the break. then the cut DNA is religated.
Suramin can inhibit cell proliferation and DNA synthesis in HeLa cells culture. It abolishes the replication of SV40 DNA completely with 40 μM concentration. DNA polymerase α is more sensitive to concentrations of suramin than DNA polymerase δ with the IC50 of 8 µM and 36 µM respectively. Suramin is a potent inhibitor of DNA strand exchange and ATPase activities of bacterial RecA proteins and RecA-catalysed proteolytic cleavage of the LexA repressor. The inhibition mechanism of suramin involves its ability to disassemble RecA–single-stranded DNA filaments.
In the animal assay, compared to control rats, treatment with suramin shows lower values for pulmonary artery pressure, right ventricular hypertrophy, and distal vessel muscularization on day 21. Suramin treatment suppresses PA-SMC proliferation and attenuates both the inflammatory response and the deposition of collagen.
References:
[1].Jindal HK, et al. Suramin affects DNA synthesis in HeLa cells by inhibition of DNA polymerases. Cancer Res. 1990 Dec 15;50(24):7754-7.
[2].Nautiyal A, et al. Suramin is a potent and selective inhibitor of Mycobacterium tuberculosis RecA protein and the SOS response: RecA as a potential target for antibacterial drug discovery. J Antimicrob Chemother. 2014 Jul;69(7):1834-43.
[3].Bojanowski K, et al. Suramin is an inhibitor of DNA topoisomerase II in vitro and in Chinese hamster fibrosarcomacells. Proc Natl Acad Sci U S A. 1992 Apr 1;89(7):3025-9.
[4].Izikki M, et al. The beneficial effect of suramin on monocrotaline-induced pulmonary hypertension in rats. PLoS One. 2013 Oct 15;8(10):e77073.
| Physical Appearance | A solid |
| Storage | Store at RT |
| M.Wt | 1429.15 |
| Cas No. | 129-46-4 |
| Formula | C51H34N6Na6O23S6 |
| Solubility | ≥71.45 mg/mL in H2O; insoluble in EtOH; ≥21 mg/mL in DMSO |
| Chemical Name | sodium 8,8'-((3,3'-((3,3'-(carbonylbis(azanediyl))bis(benzoyl))bis(azanediyl))bis(4-methylbenzoyl))bis(azanediyl))bis(naphthalene-1,3,5-trisulfonate) |
| SDF | Download SDF |
| Canonical SMILES | [O-]S(=O)(C1=C(C(NC(C2=CC=C(C)C(NC(C3=CC=CC(NC(NC4=CC(C(NC5=CC(C(NC(C(C6=CC(S([O-])(=O)=O)=C7)=C7S([O-])(=O)=O)=CC=C6S([O-])(=O)=O)=O)=CC=C5C)=O)=CC=C4)=O)=C3)=O)=C2)=O)=CC=C8S([O-])(=O)=O)C8=CC(S([O-])(=O)=O)=C1)=O.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+] |
| 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. |
Quality Control & MSDS
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Chemical structure
