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 |
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| MW: | 1429.1 |
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| Source: | Synthetic. |
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| CAS: | 129-46-4 |
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| MI: | 14: 9006 |
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| RTECS: | QM7000000 |
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| Purity: | ≥98% (HPLC) |
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| Appearance: | White to off-white solid. |
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| Solubility: | Soluble in water or physiological saline; sparingly soluble in 95% ethanol; insoluble in benzene, ether or chloroform. |
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| Shipping: | Ambient |
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| 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;
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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),
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