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Suramin . hexasodium salt

Purinergic receptor inhibitor
ALX-430-022-G001 1 g Inquire for pricing
ALX-430-022-M250 250 mg Inquire for pricing
ALX-430-022-M050 50 mg Inquire for pricing
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Replaces Prod. #: BML-G430

Polysulfonated naphthylurea. P2x and P2y purinergic receptor antagonist. Antitumor, antiangiogenic and antiparasitic compound. Inhibits sirtuin 1, sirtuin 5 and topoisomerase II. Inhibits the cell surface binding of various growth factors including PDGF, EGF, FGFa and FGFb. Blocks association of G protein α and β/γ-subunits. Potent competitive inhibitor of reverse transcriptase and protects T lymphocytes against in vitro human immunodeficiency virus infection. Potent inhibitor of melanoma heparanase and tumor cell metastasis. Selective Edg-3 antagonist.

Product Specification

Formula:C51H34N6O23S6 . 6Na
MI:14: 9006
Purity:≥98% (HPLC)
Appearance:White to off-white solid.
Solubility:Soluble in water or physiological saline; sparingly soluble in 95% ethanol; insoluble in benzene, ether or chloroform.
Long Term Storage:+4°C
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Product Literature References

Identification and characterization of novel sirtuin inhibitor scaffolds: B.D. Sanders, et al.; Bioorg. Med. Chem. 17, 7031 (2009), Abstract;
DBC1 is a negative regulator of SIRT1: J.E. Kim, et al.; Nature 451, 583 (2008), Abstract;
The Sirtuin family: therapeutic targets to treat diseases of aging: J.C. Milne & J.M. Denu; Curr. Opin. Chem. Biol. 12, 11 (2008), Abstract;
Structural basis of inhibition of the human NAD+-dependent deacetylase SIRT5 by suramin: A. Schuetz, et al.; Structure 15, 377 (2007), Abstract;
Structure-activity studies on suramin analogues as inhibitors of NAD+-dependent histone deacetylases (sirtuins): J. Trapp, et al.; ChemMedChem 2, 1419 (2007), Abstract;
Pharmacological profiles of cloned mammalian P2Y-receptor subtypes: I. von Kügelgen; Pharmacol. Ther. 110, 415 (2006), Abstract;
Regulation of SIRT 1 mediated NAD dependent deacetylation: a novel role for the multifunctional enzyme CD38: P. Aksoy, et al.; BBRC 349, 353 (2006), Abstract;
Understanding the mechanism of the antimitogenic activity of suramin: K.M. Kathir, et al.; Biochemistry 45, 899 (2006), Abstract;
Suramin disrupts receptor-G protein coupling by blocking association of G protein alpha and betagamma subunits: W.C. Chung & J.C. Kermode; J. Phamacol. Exp. Ther. 313, 191 (2005), Abstract; Full Text
Suramin inhibits death receptor-induced apoptosis in vitro and fulminant apoptotic liver damage in mice: S.T. Eichhorst, et al.; Nat. Med. 10, 602 (2004), Abstract;
Catalytic topoisomerase II inhibitors in cancer therapy: A.K. Larsen, et al.; Pharmacol. Ther. 99, 167 (2003), Abstract;
Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan: K.T. Howitz, et al.; Nature 425, 191 (2003), Abstract;
Suramin's development: what did we learn?: M. Kaur, et al.; Invest. New Drugs 20, 209 (2002), Abstract;
Fibroblast growth factors and their inhibitors: F. Manetti, et al.; Curr. Pharm. Des. 6, 1897 (2000), Abstract;
Conformational requirements of suramin to target angiogenic growth factors: P.A. Raj, et al.; Angiogenesis 2, 183 (1998), Abstract;
PPADS and suramin as antagonists at cloned P2Y- and P2U-purinoceptors: S.J. Charlton, et al.; Br. J. Pharmacol. 118, 704 (1996), Abstract;
Suramin alters phosphoinositide synthesis and inhibits growth factor receptor binding in HT-29 cells: R. Kopp & A. Pfeiffer; Cancer Res. 50, 6490 (1990), Abstract;
Suramin: a potent inhibitor of the reverse transcriptase of RNA tumor viruses: E. De Clerq; Cancer Lett. 8, 9 (1979), Abstract;

General Literature References

Differential pharmacological properties and signal transduction of the sphingosine 1-phosphate receptors EDG-1, EDG-3, and EDG-5: N. Ancellin & T. Hla; J. Biol. Chem. 274, 18997 (1999), Abstract;
Suramin. A potent inhibitor of melanoma heparanase and invasion: M. Nakajima, et al.; J. Biol. Chem. 266, 9661 (1991), Abstract;
Identification of allosteric antagonists of receptor-guanine nucleotide-binding protein interactions: R.R. Huang, et al.; Mol. Pharmacol. 37, 304 (1990), Abstract;
Inhibition of human immunodeficiency virus type I reverse transcriptase by suramin-related compounds: K.D. Jentsch, et al.; J. Gen. Virol. 68, 2183 (1987), Abstract;
Suramin inhibition of growth factor receptor binding and mitogenicity in AKR-2B cells: R.J. Coffey, et al.; J. Cell Physiol. 132, 143 (1987), Abstract;
Efficient reversion of simian sarcoma virus-transformation and inhibition of growth factor-induced mitogenesis by suramin: C. Betsholtz, et al.; Proc. Natl. Acad. Sci. USA 83, 6440 (1986), Abstract;
Suramin binds to platelet-derived growth factor and inhibits its biological activity: M. Hosang; J. Cell. Biochem. 29, 265 (1985), Abstract;
Suramin protection of T cells in vitro against infectivity and cytopathic effect of HTLV-III: H. Mitsuya, et al.; Science 226, 172 (1984), Full Text

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