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Chemical Structure| 129-46-4 Chemical Structure| 129-46-4

Structure of Suramin sodium salt
CAS No.: 129-46-4

Chemical Structure| 129-46-4

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Suramin sodium salt (Suramin hexasodium salt) is a reversible, competitive inhibitor of protein-tyrosine phosphatases (PTPases). It is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM), and also acts as a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor and efficiently inhibits IP5K. Additionally, it has antiparasitic, anti-neoplastic, and anti-angiogenic properties.

Synonyms: Suramin hexasodium salt; Suramin Sodium; NF 060

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Product Details of Suramin sodium salt

CAS No. :129-46-4
Formula : C51H34N6Na6O23S6
M.W : 1429.17
SMILES Code : O=C(NC1=CC(C(NC2=CC(C(NC3=CC=C(S(=O)([O-])=O)C4=CC(S(=O)([O-])=O)=CC(S(=O)([O-])=O)=C34)=O)=CC=C2C)=O)=CC=C1)NC5=CC(C(NC6=CC(C(NC7=CC=C(S(=O)([O-])=O)C8=CC(S(=O)([O-])=O)=CC(S(=O)([O-])=O)=C78)=O)=CC=C6C)=O)=CC=C5.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]
Synonyms :
Suramin hexasodium salt; Suramin Sodium; NF 060
MDL No. :MFCD00210217
InChI Key :VAPNKLKDKUDFHK-UHFFFAOYSA-H
Pubchem ID :8514

Safety of Suramin sodium salt

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of Suramin sodium salt

GPCR

Isoform Comparison

Biological Activity

Target
  • SIRT1

    SirT1, IC50:297 nM

  • SIRT5

    SirT5, IC50:22 μM

  • RdRp

    RdRp, IC50:0.26 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Saos-2 cells 10 –25 µM 6 weeks No telomere shortening was observed AAPS J. 2015 Jan;17(1):268-76.
DU145 cells 300 µg/ml 10 minutes To determine the effects of suramin on tyrosine phosphorylation in DU145 cells, it was found that suramin significantly increased the tyrosine phosphorylation of 75 and 135 kDa proteins. J Clin Invest. 1992 Dec;90(6):2166-74.
LNCaP cells 300 µg/ml 10 minutes To determine the effects of suramin on tyrosine phosphorylation in LNCaP cells, it was found that suramin significantly increased the tyrosine phosphorylation of 75 and 135 kDa proteins. J Clin Invest. 1992 Dec;90(6):2166-74.
Lycopersicon peruvianum suspension-cultured cells 700 µM 10 minutes Suramin inhibited the alkalinization of the medium induced by systemin, chitosan, and pmg elicitor. Proc Natl Acad Sci U S A. 2000 Aug 1;97(16):8862-7.
Monocytes 200 µM 2 days Suramin reduced the expression of FcγRI, FcγRII, FcεRII, and FcαR on monocytes and impaired their phagocytic capacity. Immunology. 1994 Apr;81(4):598-604.
Chinese hamster fibrosarcoma cells (DC-3F) 50 µM 24 hours Determine the intracellular distribution of Suramin, results showed Suramin was predominantly located in the nucleus. Proc Natl Acad Sci U S A. 1992 Apr 1;89(7):3025-9.
KB cells 300 µM 24 hours and 48 hours To investigate the effect of Suramin on the growth of KB cells, results showed that Suramin was able to sustain the growth of KB carcinoma cells cultured under serum-free conditions. J Clin Invest. 1992 Apr;89(4):1242-7.
HEK293T cells 0.02 - 5 mM 4 hours To evaluate the neutralizing effect of Suramin on SARS-CoV-2 pseudotyped viral particles, results showed that Suramin exhibited broad entry inhibition among all three variants tested (wild type, Delta, and Omicron) Commun Biol. 2023 Apr 8;6(1):387.
Vero E6 cells 5, 10, 50, 100, 1000, 10000 µM 48 hours To evaluate the cytotoxicity of Suramin on Vero E6 cells, results showed very low cytotoxicity (<20%) even at suramin concentrations up to 10 mM Commun Biol. 2023 Apr 8;6(1):387.
Lycopersicon peruvianum suspension-cultured cells 1 mM 5 minutes Suramin inhibited the activation of the 48-kDa MBP kinase induced by systemin, chitosan, and pmg elicitor. Proc Natl Acad Sci U S A. 2000 Aug 1;97(16):8862-7.
FaDu cells 10 –25 µM 6 weeks Inhibited telomerase activity, leading to gradual telomere shortening (maximum of 30%) and cell senescence AAPS J. 2015 Jan;17(1):268-76.
PC3 cells 10 –25 µM 6 weeks Inhibited telomerase activity, leading to gradual telomere shortening (maximum of 30%) and cell senescence AAPS J. 2015 Jan;17(1):268-76.
MCF7 cells 10 –25 µM 6 weeks Inhibited telomerase activity, leading to gradual telomere shortening (maximum of 30%) and cell senescence AAPS J. 2015 Jan;17(1):268-76.
A431 cells 100 µM and 300 µM 72 hours and 96 hours To investigate the effect of Suramin on EGFR in A431 cells, results showed that Suramin treatment led to a dramatic reduction in EGFR abundance and a shift in EGFR mobility, indicating Suramin-induced downregulation of EGFR. J Clin Invest. 1992 Apr;89(4):1242-7.
U937 cells 50-200 µM 8-72 hours Suramin inhibited the proliferation of U937 cells and reduced the expression of FcγRI, FcγRII, FcεRII, and FcαR. Immunology. 1994 Apr;81(4):598-604.
U-266 cells 30 µM 90 minutes Suramin inhibited the binding of 125I-IL-6 to U-266 cells, with a half-maximal inhibition concentration of 30 μM J Clin Invest. 1993 Nov;92(5):2152-9.
MCF-7 cells 300 µM 90 minutes Suramin inhibited the binding of 125I-TNFα to MCF-7 cells, with a half-maximal inhibition concentration of 300 μM J Clin Invest. 1993 Nov;92(5):2152-9.
PC3 cells 300 µg/ml seconds To determine the effects of suramin on tyrosine phosphorylation in PC3 cells, it was found that suramin significantly increased the tyrosine phosphorylation of several distinct proteins. J Clin Invest. 1992 Dec;90(6):2166-74.
U2OS cells 62.5 to 500 µM Suramin at 62.5 μM accumulated p27 and CDT1, and at 250-500 μM accumulated Nrf2, indicating that Suramin inhibits CRL-mediated ubiquitination, leading to the accumulation of CRL substrates. Proc Natl Acad Sci U S A. 2016 Apr 5;113(14):E2011-8.
B-9 cells 30 µM Suramin inhibited the proliferation of B-9 cells in response to IL-6, with a half-maximal inhibition concentration of 30 μM J Clin Invest. 1993 Nov;92(5):2152-9.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice FaDu tumor model Intravenous injection 10 mg/kg Twice a week for 6 weeks Resulted in telomere shortening of >40% in tumor cells AAPS J. 2015 Jan;17(1):268-76.
Mice Pkd1-deficient mouse model Intraperitoneal injection 60 mg/kg Twice a week for 8 weeks Suramin significantly reduced renal cyst densities, cell proliferation, and macrophage infiltration, but did not improve kidney function Int J Mol Sci. 2022 Jul 31;23(15):8499
Tomato plants 14-day-old tomato plants Supplied through cut stems 700 µM 1-hour pretreatment Suramin inhibited the synthesis of serine proteinase inhibitors I and II induced by systemin and completely inhibited the synthesis of inhibitors induced by wounding. Proc Natl Acad Sci U S A. 2000 Aug 1;97(16):8862-7.
BALB/c X DBA/2 (CD)F1 mice C-26 adenocarcinoma model Intraperitoneal injection 75 mg/kg Injected on days 7 and 12 Suramin significantly improved weight loss in C-26 adenocarcinoma model mice, reducing muscle and fat tissue wasting and hypoglycemia J Clin Invest. 1993 Nov;92(5):2152-9.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00001230 - Recruiting - United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Recruiting Bethesda, Maryland, United States, 20892 Contact: For more information at the NIH Clinical Center contact Office of Patient Recruitment (OPR)    800-441-1222 ext TTY8864111010    prpl@cc.nih.gov Less <<
NCT02347332 Recurrent or Metastatic Head a... More >>nd Neck Carcinoma Less << Phase 3 Active, not recruiting June 2018 -
NCT02871284 Exercise Chem... More >>otherapy-induced Polyneuropathy Less << Phase 2 Phase 3 Recruiting December 2019 Germany ... More >> National Center for Tumor Diseases Recruiting Heidelberg, Germany, 69120 Contact: Joachim Wiskemann, Dr.       joachim.wiskemann@nct-heidelberg.de    Contact: Jana Müller       jana.mueller@nct-heidelberg.de Less <<
NCT00003038 Adrenocortical Carcinoma ... More >> Breast Cancer Colorectal Cancer Prostate Cancer Unspecified Adult Solid Tumor, Protocol Specific Less << Phase 1 Completed - United States, Minnesota ... More >> Mayo Clinic Cancer Center Rochester, Minnesota, United States, 55905 Less <<
NCT00001266 Prostatic Neoplasm Phase 2 Completed - United States, Maryland ... More >> National Cancer Institute (NCI) Bethesda, Maryland, United States, 20892 Less <<
NCT00006476 Bladder Cancer Phase 1 Completed - United Kingdom ... More >> Oxford Radcliffe Hospital Oxford, England, United Kingdom, 0X3 9DU Less <<
NCT00004073 Brain and Central Nervous Syst... More >>em Tumors Less << Phase 2 Completed - United States, Alabama ... More >> University of Alabama Comprehensive Cancer Center Birmingham, Alabama, United States, 35294 United States, Florida H. Lee Moffitt Cancer Center and Research Institute Tampa, Florida, United States, 33612 United States, Georgia Emory University Hospital - Atlanta Atlanta, Georgia, United States, 30322 United States, Maryland Johns Hopkins Oncology Center Baltimore, Maryland, United States, 21231 United States, Massachusetts Massachusetts General Hospital Cancer Center Boston, Massachusetts, United States, 02114 United States, Michigan Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, North Carolina Comprehensive Cancer Center of Wake Forest University Baptist Medical Center Winston-Salem, North Carolina, United States, 27157-1082 United States, Pennsylvania University of Pennsylvania Cancer Center Philadelphia, Pennsylvania, United States, 19104 United States, Texas University of Texas Health Science Center at San Antonio San Antonio, Texas, United States, 78284-7811 Less <<
NCT00001381 Bladder Neoplasms ... More >> Carcinoma, Transitional Cell Less << Phase 1 Completed - United States, Maryland ... More >> National Cancer Institute (NCI) Bethesda, Maryland, United States, 20892 Less <<
NCT00002881 Prostate Cancer Phase 3 Completed - United States, District of Col... More >>umbia Walter Reed Army Medical Center Washington, District of Columbia, United States, 20307-5000 Less <<
NCT00006929 Recurrent Non-small Cell Lung ... More >>Cancer Stage IIIB Non-small Cell Lung Cancer Stage IV Non-small Cell Lung Cancer Less << Phase 2 Completed - United States, Ohio ... More >> Arthur G. James Cancer Hospital and Solove Research Institute at Ohio State University Medical Center Columbus, Ohio, United States, 43210 Less <<
NCT00002639 Brain and Central Nervous Syst... More >>em Tumors Less << Phase 2 Completed - United States, Georgia ... More >> Department of Neurosurgery - Emory Atlanta, Georgia, United States, 30322 Less <<
NCT01671332 Carcinoma, Non Small Cell Lung Phase 2 Unknown December 2016 United States, Wisconsin ... More >> University of Wisconsin Carbone Comprehensive Cancer Center Madison, Wisconsin, United States, 53792 Medical College of Wisconsin Milwaukee, Wisconsin, United States Less <<
NCT00002652 Multiple Myeloma and Plasma Ce... More >>ll Neoplasm Less << Phase 2 Completed - United States, Arkansas ... More >> University of Arkansas for Medical Sciences Little Rock, Arkansas, United States, 72205 Less <<
NCT00083109 Recurrent Renal Cell Carcinoma... More >> Stage IV Renal Cell Cancer Less << Phase 1 Phase 2 Completed - United States, Ohio ... More >> Cleveland Clinic Foundation Cleveland, Ohio, United States, 44195 Less <<
NCT00054028 Recurrent Breast Cancer ... More >> Stage IIIB Breast Cancer Stage IV Breast Cancer Less << Phase 1 Phase 2 Completed - United States, Ohio ... More >> Ohio State University Medical Center Columbus, Ohio, United States, 43210 Less <<
NCT00066768 Recurrent Non-small Cell Lung ... More >>Cancer Stage IIIB Non-small Cell Lung Cancer Stage IV Non-small Cell Lung Cancer Less << Phase 1 Completed - United States, Ohio ... More >> Ohio State University Medical Center Columbus, Ohio, United States, 43210 Less <<
NCT01038752 Non-small Cell Lung Cancer Phase 2 Terminated - United States, Illinois ... More >> John H Stroger Jr Hospital of Cook County Chicago, Illinois, United States, 60612 United States, Virginia Virginia Commonwealth University Massey Cancer Center Richmond, Virginia, United States, 23298 Less <<
NCT00054028 - Completed - -
NCT02508259 Autism Spectrum Disorders Phase 1 Phase 2 Completed - United States, California ... More >> University of California, San Diego School of Medicine La Jolla, California, United States, 92093 Less <<
NCT01038752 - Terminated - -
NCT00002921 Adrenocortical Carcinoma Phase 2 Terminated(Permanently Closed ... More >>Due to Lack of Accrual) Less << - -
NCT00002723 Prostate Cancer Phase 3 Completed - -
NCT06058962 Autism Spectrum Disorder PHASE2 COMPLETED 2021-03-15 PaxMedica, Tarrytown, New York... More >>, 10591, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.70mL

0.14mL

0.07mL

3.50mL

0.70mL

0.35mL

7.00mL

1.40mL

0.70mL

References

 

Historical Records

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