Aurothiomalate disodium
Aurothiomalate disodium acts as an inhibitor of PKCI and TrxR1. Aurothiomalate disodium disrupts the PKCI-Par6-Rac1 signaling pathway, and also inhibits TrxR1 activity, TNFα-induced NF-κB activation, and the expression of pro-inflammatory genes. Aurothiomalate disodium blocks Kras-mediated BASC expansion and lung tumor growth, inhibits anchorage-independent growth and tumorigenicity of lung cancer cells, and suppresses neutrophil chemotaxis, phagocytosis, and leukocyte extravasation. Aurothiomalate disodium can be used in research related to rheumatoid arthritis and non-small cell lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 74916-57-7
- Formula: C4H3AuNa2O4S
- Molecular Weight:390.08
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PKCι |
Aurothiomalate (20 μmol/L; in vitro culture duration) disodium blocks the proliferative expansion and morphological transformation of bronchoalveolar stem cells isolated from LSL-Kras mice that are mediated by oncogenic Kras in vitro[2].
Aurothiomalate disodium potently inhibits the activity of mouse liver thioredoxin reductase in vitro[3].
Aurothiomalate (25-50 μM; administered 48 h prior to 6 h TNFα stimulation) disodium inhibits TNFα-induced NF-κB-dependent gene expression in TrxR1-overexpressing COS7 cells in a dose-dependent manner[3].
Aurothiomalate (50 μM; administered 48 h prior to TNFα stimulation) disodium inhibits TNFα-induced NF-κB DNA-binding activity in TrxR1-overexpressing COS7 cells[3].
Aurothiomalate (25 μM; administered concurrently with TNFα stimulation for 6 h) disodium inhibits TNFα-induced expression of the NF-κB-targeted pro-inflammatory genes E-selectin and COX-2 in bovine arterial endothelial cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Bovine arterial endothelial cells (BAEC)
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Concentration:25 uM
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Incubation Time:6 hours
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Result:Suppressed TNFa-induced NF-kB-dependent gene expression in a dose-dependent manner.
Did not affect TrxR1 mRNA level in COS7 cells.
Aurothiomalate (0.7 μg/g body weight; administered via intravenous injection, intramuscular injection, or direct air pouch injection; dosed twice) disodium significantly reduces the leukocyte count in exudate in carrageenan-induced acute inflammation models in mice, with intravenous injection exerting the strongest inhibitory effect[4].
Aurothiomalate (0.7 μg/g body weight; tail vein injection; single administration) disodium significantly reduces the leukocyte count in exudate in a carrageenan-induced acute inflammation mouse model[4].
Aurothiomalate (0.7 μg/g body weight; intravenous injection, intramuscular injection, direct air pouch injection) disodium significantly inhibits phagocytosis and chemotaxis of neutrophils in carrageenan-induced acute inflammation in mice, with intravenous and intramuscular injections exerting stronger inhibitory effects on chemotaxis than direct air pouch injection[4].
Aurothiomalate (2-60 mg/kg; intramuscular injection; daily administration) disodium exerts potent antitumor activity against A427 lung cancer xenografts by inhibiting cell proliferation and the Mek/Erk signaling pathway[6].
Aurothiomalate (20-60 mg/kg; intramuscular injection; daily) disodium exhibits moderate antitumor activity against H460 lung cancer xenografts by inhibiting cell proliferation and the Mek/Erk signaling pathway[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nude mice (Harlan Sprague-Dawley, female, 4-6 weeks old, subcutaneous xenograft model via injection of human H460 lung cancer cells)[6]
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Dosage:20 mg/kg; 60 mg/kg
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Administration:i.m.; daily
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Result:Caused a statistically significant ~50% reduction in H460 tumor volume compared to controls at the 60 mg/kg dose.
Reduced BrdUrd-positive nuclei (proliferative index) from ~21% in controls to ~11% at the 60 mg/kg dose.
Reduced the ratio of phospho-Erk 1,2 to total Erk 1,2 compared to controls at the 60 mg/kg dose.
Did not significantly increase the apoptotic index (TUNEL-positive cells remained <1%) or alter tumor vascularization (PECAM1 staining/expression unchanged) at either dose.
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Animal Model:Athymic nude mice (Harlan Sprague-Dawley, female, 4-6 weeks old, subcutaneous xenograft model via injection of human A427 lung cancer cells)[6]
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Dosage:2 mg/kg; 6 mg/kg; 20 mg/kg; 60 mg/kg
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Administration:i.m.; daily
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Result:Caused statistically significant inhibition of A427 tumor growth, with final tumor volume far lower than control tumors.
Reduced BrdUrd-positive nuclei (proliferative index) from ~17% in controls to ~9% at 2 mg/kg, ~6% at 6 mg/kg, ~5% at 20 mg/kg, and ~9% at 60 mg/kg.
Reduced the ratio of phospho-Erk 1,2 to total Erk 1,2 compared to controls.
Did not significantly increase the apoptotic index (TUNEL-positive cells remained <1%) or alter tumor vascularization (PECAM1 staining/expression unchanged) at any dose.
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Animal Model:KrasLA2 (3-week-old; spontaneous activation of latent oncogenic KrasG12D allele via somatic recombination)[2]
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Dosage:60 mg/kg
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Administration:i.p.; daily; 3 weeks; 6 weeks
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Result:Blocked the significant increase in BASCs per terminal bronchiole seen in saline-treated KrasLA2 mice, with BASC number and distribution matching levels in nontransgenic mice.
Reduced lung tumor growth, with a mean fold-change in average tumor size of ~1.6, compared to ~2.5 in saline-treated mice.
Chemical Information
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CAS No. 74916-57-7
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Molecular Weight 390.08
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Formula C4H3AuNa2O4S
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SMILES
O=C(CC(C([O-])=O)[S-])[O-].[Na+].[Au+].[Na+]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Campbell JM, et al. Action of sodium aurothiomalate on erythrocyte membrane. Ann Rheum Dis. 1992;51(8):969-971. [Content Brief]
[3]. Sakurai A, et al. Overexpression of thioredoxin reductase 1 regulates NF-kappa B activation. J Cell Physiol. 2004;198(1):22-30. [Content Brief]
[4]. Sin YM, et al. Effect of sodium aurothiomalate on carrageenan induced inflammation of the air pouch in mice. Ann Rheum Dis. 1992;51(1):112-116. [Content Brief]
[5]. Lewis D, et al. Gold levels produced by treatment with auranofin and sodium aurothiomalate. Ann Rheum Dis. 1983;42(5):566-570. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Aurothiomalate disodium Related Classifications
HY-W010270A Related Classifications
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