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Auranofin (Synonyms: SKF-39162)

Cat. No.: HY-B1123 Purity: >98.0%
Data Sheet SDS Handling Instructions

Auranofin (SKF-39162) is a thioredoxin reductase (TrxR) inhibitor with an IC50 of 0.2 μM.

For research use only. We do not sell to patients.
Auranofin Chemical Structure

Auranofin Chemical Structure

CAS No. : 34031-32-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO $55 In-stock
10 mg $50 In-stock
50 mg $80 In-stock
100 mg $130 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Auranofin (SKF-39162) is a thioredoxin reductase (TrxR) inhibitor with an IC50 of 0.2 μM.

IC50 & Target

IC50: 0.2 μM (TrxR)[1]

In Vitro

Auranofin is a drug that is approved for the treatment of rheumatoid arthritis but is being investigated for potential therapeutic application in a number of other diseases including cancer, neurodegenerative disorders. Auranofin induces apoptosis in cells through a Bax/Bak-dependent mechanism associated with selective disruption of mitochondrial redox homeostasis in conjunction with oxidation of Prx3[1]. Auranofin inhibits proliferation and survival of SKOV3 cells in a dose- and time-dependent manner. Auranofin treatment activates the pro-apoptotic caspase-3, increases protein levels of apoptosis-inducing proteins Bax and Bim and reduces the expression of the anti-apoptotic mediator Bcl-2 in SKOV3 cells[2]. Auranofin is a lipophilic gold compound with anti-inflammatory and immunosuppressive properties. Auranofin inhibits the cell growth and induction of mitochondrial apoptosis in PC3 human prostate cancer cells. Treatment with auranofin significantly inhibits cell viability with an IC50 value of 2.5 μM after 24 h[3].

In Vivo

Prophylactic treatment of adjuvant-induced arthritis rats with auranofin results in a slight reduction in paw edema, a complete normalization of the depressed IL-2 production, and a reduction of the elevated IL-1 production, but has no effect on the depressed IL-3 production[4].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02176135 Vaccine and Gene Therapy Institute, Florida|University of Miami HIV Phase 1|Phase 2
NCT02089048 National Institute of Allergy and Infectious Diseases (NIAID) Amoebiasis April 2, 2014 Phase 1
NCT01747798 Mayo Clinic Recurrent Fallopian Tube Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Primary Peritoneal Cavity Cancer November 2012
NCT01419691 University of Kansas Medical Center|The Leukemia and Lymphoma Society|Kansas Bioscience Authority|Therapeutics for Rare and Neglected Diseases (TRND) Chronic Lymphocytic Leukemia (CLL)|Small Lymphocytic Lymphoma|Leukemia, Prolymphocytic September 2011 Phase 2
NCT02063698 Mayo Clinic|National Cancer Institute (NCI) Pain February 2014
NCT02126527 Mayo Clinic|National Cancer Institute (NCI) Recurrent Non-small Cell Lung Cancer|Unspecified Adult Solid Tumor, Protocol Specific August 2013 Phase 1
NCT02736968 National Institute of Allergy and Infectious Diseases (NIAID) Amoebic Dysentery|Giardiasis August 19, 2016 Phase 2
NCT01737502 Mayo Clinic|National Cancer Institute (NCI) Extensive Stage Small Cell Lung Carcinoma|Lung Adenocarcinoma|Recurrent Non-Small Cell Lung Carcinoma|Recurrent Small Cell Lung Carcinoma|Squamous Cell Lung Carcinoma|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IV Non-Small Cell Lung Cancer November 2012 Phase 1|Phase 2
NCT02961829 Federal University of São Paulo|Fundação de Amparo à Pesquisa do Estado de São Paulo|Conselho Nacional de Desenvolvimento Científico e Tecnológico|ViiV Healthcare Chronic Infection|HIV July 2015
NCT02968927 The Aurum Institute NPC Tuberculosis November 2016 Phase 2
NCT02770378 University of Ulm|Reliable Cancer Therapies|Anticancer Fund, Belgium Glioblastoma November 2016 Phase 1
NCT02176135 Vaccine and Gene Therapy Institute, Florida|University of Miami HIV Phase 1|Phase 2
NCT02089048 National Institute of Allergy and Infectious Diseases (NIAID) Amoebiasis April 2, 2014 Phase 1
NCT01747798 Mayo Clinic Recurrent Fallopian Tube Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Primary Peritoneal Cavity Cancer November 2012
NCT01419691 University of Kansas Medical Center|The Leukemia and Lymphoma Society|Kansas Bioscience Authority|Therapeutics for Rare and Neglected Diseases (TRND) Chronic Lymphocytic Leukemia (CLL)|Small Lymphocytic Lymphoma|Leukemia, Prolymphocytic September 2011 Phase 2
NCT02063698 Mayo Clinic|National Cancer Institute (NCI) Pain February 2014
NCT02126527 Mayo Clinic|National Cancer Institute (NCI) Recurrent Non-small Cell Lung Cancer|Unspecified Adult Solid Tumor, Protocol Specific August 2013 Phase 1
NCT02736968 National Institute of Allergy and Infectious Diseases (NIAID) Amoebic Dysentery|Giardiasis August 19, 2016 Phase 2
NCT01737502 Mayo Clinic|National Cancer Institute (NCI) Extensive Stage Small Cell Lung Carcinoma|Lung Adenocarcinoma|Recurrent Non-Small Cell Lung Carcinoma|Recurrent Small Cell Lung Carcinoma|Squamous Cell Lung Carcinoma|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IV Non-Small Cell Lung Cancer November 2012 Phase 1|Phase 2
NCT02961829 Federal University of São Paulo|Fundação de Amparo à Pesquisa do Estado de São Paulo|Conselho Nacional de Desenvolvimento Científico e Tecnológico|ViiV Healthcare Chronic Infection|HIV July 2015
NCT02968927 The Aurum Institute NPC Tuberculosis November 2016 Phase 2
NCT02770378 University of Ulm|Reliable Cancer Therapies|Anticancer Fund, Belgium Glioblastoma November 2016 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.4695 mL 7.3475 mL 14.6951 mL
5 mM 0.2939 mL 1.4695 mL 2.9390 mL
10 mM 0.1470 mL 0.7348 mL 1.4695 mL
Cell Assay
[2]

Auranofin is dissolved in DMSO. Cells are treated with auranofin (0, 50, 100, 200 and 400 nM) for 72 h for the dose-dependent response assay and 100 nM of auranofin is added into the wells for 0, 24, 72 and 120 h for the time-dependent response assay. Control cultures are treated with DMSO. Cell viability is measured by the MTT assay[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

Rat: Prophylactically, auranofin (6.7 to 15 mg of gold/kg), indomethacin (2 mg/kg) or tragacanth vehicle control were administered orally at daily intervals beginning on the day of adjuvant injection. On days 16 to 17 peritoneal exudate cells or spleen cells from normal or adjuvant-injected rats were isolated and tested[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

680.5

Formula

C₂₀H₃₆AuO₉PS

CAS No.

34031-32-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: >98.0%

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Auranofin
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HY-B1123
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