Aurothiomalate sodium

Name: Aurothiomalate sodium
Brand: MedChemExpress
SKU: HY-106381
Rating: 4.5 (0 reviews)

製品番号: HY-106381 純度: 98.0%: Data Sheet SDS COA 取扱説明書
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Aurothiomalate sodium is the tetrameric form of Aurothiomalate sodium (HY-106381). Aurothiomalate sodium acts as an inhibitor of PKCI and TrxR1. Aurothiomalate sodium 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 sodium 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 sodium can be used in research related to rheumatoid arthritis and non-small cell lung cancer.

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Aurothiomalate sodium 構造式

CAS 番号 : 12244-57-4

容量	価格（税別）	在庫状況	数量
5 mg	$60	在庫あり	Estimated Time of Arrival: December 31
10 mg	$90	在庫あり	Estimated Time of Arrival: December 31
25 mg	$180	在庫あり	Estimated Time of Arrival: December 31
50 mg	$280	在庫あり	Estimated Time of Arrival: December 31
100 mg	$450	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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カスタマーレビュー

Based on 0 publication(s) in Google Scholar

Other Forms of Aurothiomalate sodium:

Aurothiomalate tetramer sodium 在庫あり
Aurothiomalate disodium お問い合わせ

TrxR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

TrxR1 TrxR2

NF-κB アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

PKC アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]^[2]

PKCι

体外実験

Aurothiomalate sodium (20 μmol/L; in vitro culture duration) 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 sodium potently inhibits the activity of mouse liver thioredoxin reductase in vitro^[3].
Aurothiomalate sodium (25-50 μM; administered 48 h prior to 6 h TNFα stimulation) inhibits TNFα-induced NF-κB-dependent gene expression in TrxR1-overexpressing COS7 cells in a dose-dependent manner^[3].
Aurothiomalate sodium (50 μM; administered 48 h prior to TNFα stimulation) inhibits TNFα-induced NF-κB DNA-binding activity in TrxR1-overexpressing COS7 cells^[3].
Aurothiomalate sodium (25 μM; administered concurrently with TNFα stimulation for 6 h) 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.

Western Blot Analysis^[1]

Cell Line:	Bovine arterial endothelial cells (BAEC)
Concentration:	25 uM
Incubation Time:	6 hours
Result:	Suppressed TNFa-induced NF-kB-dependent gene expression in a dose-dependent manner. Did not affect TrxR1 mRNA level in COS7 cells.

体内実験

Aurothiomalate sodium (intraperitoneal injection; administered daily for 3-6 weeks at a dose of 60 mg/kg) inhibits Kras-mediated BASC expansion and reduces lung tumor growth by approximately 36% in Kras^LA2 mice^[2].
Aurothiomalate sodium (0.7 μg/g body weight; administered via intravenous injection, intramuscular injection, or direct air pouch injection; dosed twice) 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 sodium (0.7 μg/g body weight; tail vein injection; single administration) significantly reduces the leukocyte count in exudate in a carrageenan-induced acute inflammation mouse model^[4].
Aurothiomalate sodium (0.7 μg/g body weight; intravenous injection, intramuscular injection, direct air pouch injection) 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 sodium (2-60 mg/kg; intramuscular injection; daily administration) exerts potent antitumor activity against A427 lung cancer xenografts by inhibiting cell proliferation and the Mek/Erk signaling pathway^[6].
Aurothiomalate sodium (20-60 mg/kg; intramuscular injection; daily) 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.

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]
Dosage:	20 mg/kg; 60 mg/kg
Administration:	i.m.; daily
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.

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]
Dosage:	2 mg/kg; 6 mg/kg; 20 mg/kg; 60 mg/kg
Administration:	i.m.; daily
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.

Animal Model:	KrasLA2 (3-week-old; spontaneous activation of latent oncogenic KrasG12D allele via somatic recombination)^[2]
Dosage:	60 mg/kg
Administration:	i.p.; daily; 3 weeks; 6 weeks
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.

分子式

C₄H₆O₄S.Au.xNa

CAS 番号

12244-57-4

Appearance

Solid

Color

Off-white to light yellow

SMILES

OC(CC(S)C(O)=O)=O.[Na].[Au]

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

H₂O : 250 mg/mL (Need ultrasonic)

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一般には略語で表示されます：C₁V₁ = C₂V₂

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体内:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL; Clear solution; Need ultrasonic

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This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

純度とドキュメンテーション

純度: 98.0%

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データシート (299 KB) SDS (393 KB)

COA (249 KB) HNMR (260 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Campbell JM, et al. Action of sodium aurothiomalate on erythrocyte membrane. Ann Rheum Dis. 1992;51(8):969-971. [Content Brief]

[2]. Regala RP, et al. Atypical protein kinase C{iota} is required for bronchioalveolar stem cell expansion and lung tumorigenesis. Cancer Res. 2009 Oct 1;69(19):7603-11.

[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]

[6]. Regala RP, et al. Atypical protein kinase C iota expression and aurothiomalate sensitivity in human lung cancer cells. Cancer Res. 2008 Jul 15;68(14):5888-95.