Suramin . hexasodium salt

Specifications / Handling

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Product Details
Synonyms	Germanin; NSC 34936; SK 24728
Product Type	Chemical
Properties
Formula	C₅₁H₃₄N₆O₂₃S₆ . 6Na
MW	1291.2 . 137.9
Merck Index	14: 9006
CAS	129-46-4
RTECS	QM7000000
Source/Host Chemicals	Synthetic.
Purity Chemicals	≥98% (Pharmaceutical Grade).
Appearance	White to off-white powder.
Solubility	Soluble in water (50mM) or DMSO (10mM). Sparingly soluble in ethanol.
Other Product Data	Water Content (by Karl Fischer): ≤15%
InChi Key	VAPNKLKDKUDFHK-UHFFFAOYSA-H
Smiles	[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].CC1=CC=C(C=C1NC(=O)C1=CC(NC(=O)NC2=CC=CC(=C2)C(=O)NC2=C(C)C=CC(=C2)C(=O)NC2=C3C(C=C(C=C3S([O-])(=O)=O)S([O-])(=O)=O)=C(C=C2)S([O-])(=O)=O)=CC=C1)C(=O)NC1=CC=C(C2=C1C(=CC(=C2)S([O-])(=O)=O)S([O-])(=O)=O)S([O-])(=O)=O
Shipping and Handling
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	+4°C
Handling Advice	Keep cool and dry.
Use/Stability	Stable for at least 2 years after receipt when stored at +4°C.
Documents
MSDS	Download PDF
Product Specification Sheet
Datasheet	Download PDF

Product-specific References

Description

Potent ATPase inhibitor [1].
Potent competitive inhibitor of reverse transcriptase. Shows anti-HIV activity [2, 3].
Anticancer compound [4, 5, 15].
Protein kinase C (PKC) inhibitor [4].
Potent inhibitor of melanoma heparanase and tumor cell metastasis [6].
Non-specific growth factors inhibitor (including PDGF, EGF, aFGF and bFGF) [7, 16].
TGF-β1 inhibitor [8].
Topoisomerase I and II inhibitor [9].
Interleukin-1 (IL-1) inhibitor [10].
Interleukin-4 (IL-4) inhibitor [11].
G protein inhibitor [12].
P2X and P2Y purinergic receptor antagonist [13].
Antiangiogenic. Potent VEGF inhibitor [14, 15].
Telomerase inhibitor [17].
Shows adjuvant properties [18].
Regulates ryanodine receptor [19].
Direct adenylyl cyclase inhibitor [20].
Protein synthesis inhibitor [21].
SIRT1 (sirtuin 1) and SIRT5 (sirtuin 5) inhibitor [22, 23].
Immunosuppressive [24].
Antifibrotic agent [25].
Antiparasitic. Antiprotozoal. Athelmintic [26].
Cullin-RING E3 ubiquitin ligase inhibitor [29].
Inhibitor of the STING pathway via the inhibition of cGAMP synthase (cGAS) enzymatic activity [32].
Inhibits SARS-CoV-2 infection in cell culture by blocking early steps (binding/fusion) of the replication cycle. Potentially binds and inhibits nsp12 of SARS-CoV-2, binding to motifs harbouring the RNA-dependent RNA polymerases (RdRps) activity [34, 36].
Inhibits several dsDNA-binding proteins, including cGAS (inhibiting cGAS-STING and TLR9 mediated inflammatory responses), Mcm1040 and DNA topoisomerase II, and most recently also the AIM2 inflammasome. Effective inhibitor of dsDNA-induced inflammation [38].

Product References

Suramin: a potent ATPase inhibitor which acts on the inside surface of the sodium pump: P.A. Fortes, et al.; Biochim. Biophys. Acta 318, 262 (1973)
Suramin: a potent inhibitor of the reverse transcriptase of RNA tumor viruses: E. De Clerq; Cancer Lett. 8, 9 (1979)
Suramin protection of T cells in vitro against infectivity and cytopathic effect of HTLV-III: H. Mitsuya, et al.; Science 226, 172 (1984)
Suramin, an anti-cancer drug, inhibits protein kinase C and induces differentiation in neuroblastoma cell clone NB2A: C.E. Hensey, et al.; FEBS Lett. 258, 156 (1989)
Suramin: prototype of a new generation of antitumor compounds: R.V. La Rocca, et al.; Cancer Cells 2, 106 (1990) (Review)
Suramin. A potent inhibitor of melanoma heparanase and invasion: M. Nakajima, et al.; J. Biol. Chem. 266, 9661 (1991)
Nature of the interaction of growth factors with suramin: C.R. Middaugh, et al.; Biochemistry 31, 9016 (1992)
The antiproliferative effect of suramin on the cancer cell line SW-13 is mediated by the inhibition of transforming growth factor beta 1 (TGF-beta 1): R. Danesi, et al.; Pharmacol. Res. 25, 17 (1992)
Suramin inhibits DNA damage in human prostate cancer cells treated with topoisomerase inhibitors in vitro: H. Yamazaki, et al.; Prostate 23, 25 (1993)
Suramin blocks the binding of interleukin-1 to its receptor and neutralizes IL-1 biological activities: G. Strassmann, et al.; Int. J. Immunopharmacol. 16, 931 (1994)
Suramin blocks binding of interleukin-4 to its receptors on human tumor cells and interleukin-4-induced mitogenic response: P. Leland, et al.; Oncol. Res. 7, 227 (1995)
Suramin analogues as subtype-selective G protein inhibitors: M. Freissmuth, et al.; Mol. Pharmacol. 49, 602 (1996)
PPADS and suramin as antagonists at cloned P2Y- and P2U-purinoceptors: S.J. Charlton, et al.; Br. J. Pharmacol. 118, 704 (1996)
Suramin is a potent inhibitor of vascular endothelial growth factor. A contribution to the molecular basis of its antiangiogenic action: J. Waltenberger, et al.; J. Mol. Cell Cardiol. 28, 1523 (1996)
Antiangiogenic and antiproliferative activity of suramin analogues: A.R. Gagliardi, et al.; Cancer Chemother. Pharmacol. 41, 117 (1998)
Suppression of myocardial inflammation using suramin, a growth factor blocker: T. Shiono, et al.; Circ. J. 66, 385 (2002)
Suramin suppresses growth, alkaline-phosphatase and telomerase activity of human osteosarcoma cells in vitro: K. Trieb & H. Blahovec; Int. J. Biochem. Cell Biol. 35, 1066 (2003)
Suramin has adjuvant properties and promotes expansion of antigen-specific Th1 and Th2 cells in vivo: M. Denkinger, et al.; Int. Immunopharmacol. 4, 15 (2004)
Functional regulation of the cardiac ryanodine receptor by suramin and calmodulin involves multiple binding sites: A.P. Hill, et al; Mol. Pharmacol. 65, 1258 (2004)
Modulation of adenylyl cyclase activity in young and adult rat brain cortex. Identification of suramin as a direct inhibitor of adenylyl cyclase: J. Stöhr, et al.; J. Cell Mol. Med. 9, 940 (2005)
Inhibition by suramin of protein synthesis in vitro. Ribosomes as the target of the drug: M. Brigotti, et al.; Biochimie 88, 497 (2006)
Structure-activity studies on suramin analogues as inhibitors of NAD+-dependent histone deacetylases (sirtuins): J. Trapp, et al.; ChemMedChem 2, 1419 (2007)
Structural basis of inhibition of the human NAD+-dependent deacetylase SIRT5 by suramin: A. Schuetz, et al.; Structure 15, 377 (2007)
Suramin inhibits the CD40-CD154 costimulatory interaction: a possible mechanism for immunosuppressive effects: E. Margolles-Clark, et al.; Biochem. Pharmacol. 77, 1236 (2009)
Tissue protective and anti-fibrotic actions of suramin: new uses of an old drug: N. Liu & S. Zhuang; Curr. Clin. Pharmacol. 6, 137 (2011) (Review)
The trypanocidal drug suramin and other trypan blue mimetics are inhibitors of pyruvate kinases and bind to the adenosine site: H.P. Morgan, et al.; J. Biol. Chem. 286, 31232 (2011)
Neutralization of Apis mellifera bee venom activities by suramin: C.Z. El-Kik, et al.; Toxicon 67, 55 (2013)
Suramin inhibits helicase activity of NS3 protein of dengue virus in a fluorescence-based high throughput assay format: C. Basavannacharya & S.G. Vasudevan; BBRC 453, 539 (2014)
Suramin inhibits cullin-RING E3 ubiquitin ligases: K. Wu, et al.; PNAS 113, E2011 (2016)
Suramin is a potent inhibitor of Chikungunya and Ebola virus cell entry: L. Henss, et al.; Virol. J. 13, 149 (2016)
Suramin is a novel competitive antagonist selective to α1β2γ2 GABAA over ρ1 GABAC receptors: H. Luo, et al.; Neuropharmacol. 141, 148 (2018)
Suramin potently inhibits cGAMP synthase, cGAS, in THP1 cells to modulate IFN-β levels: M. Wang, et al.; Future Med. Chem. 10, 1301 (2018)
Evaluating the impact of suramin additive on CHO cells producing Fc-fusion protein: J.-H. Lim, et al.; Biotechnol. Lett. 41, 1255 (2019)
Suramin inhibits SARS-CoV-2 infection in cell culture by interfering 2 with early steps of the replication cycle: C. Salgado, et al.; Antimicrob. Agents Chemother. 64, e00900 (2020)
100 Years of Suramin: N. Wiedemar, et al.; Antimicr. Agents Chemother. 64, e01168-19 (2020) (Review)
Suramin, Penciclovir and Anidulafungin bind nsp12, which governs the RNA-dependent-RNA polymerase activity of SARS-CoV-2, with higher interaction energy than Remdesivir, indicating potential in the treatment of Covid-19 infection: S.K. Dey, et al.; J. Biomol. Struct. Dyn. 40, 14067 (2022)
High Throughput Screening Targeting the Dengue NS3-NS5 Interface Identifies Antivirals against Dengue, Zika and West Nile Viruses: S.N.Y. Yang, et al.; Cells 11, 730 (2022)
Discovery of an inhibitor of DNA-driven inflammation that preferentially targets the AIM2 inflammasome: J.P. Green, et al.; iScience 26, 106758 (2023)

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