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金硫丁二钠 /Aurothiomalate sodium {[allProObj[0].p_purity_real_show]}

货号:A429214 同义名: 金硫丁二酸钠 Ambeed 开学季,买赠积分,赢豪礼

Aurothiomalate sodium是一种有效的 PKCι 和硫氧还蛋白还原酶 (TrxR) 抑制剂,常用于肿瘤细胞增殖和抗风湿药物的研究,具有抗肿瘤活性。

Aurothiomalate sodium 化学结构 CAS号:12244-57-4
Aurothiomalate sodium 化学结构
CAS号:12244-57-4
Aurothiomalate sodium 3D分子结构
CAS号:12244-57-4
Aurothiomalate sodium 化学结构 CAS号:12244-57-4
Aurothiomalate sodium 3D分子结构 CAS号:12244-57-4
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Aurothiomalate sodium 纯度/质量文件 产品仅供科研

货号:A429214 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 PKC PKCα PKCβ PKCγ PKCδ PKCε PKCζ PKCη PKCθ 其他靶点 纯度
Daphnetin +

PKC, IC50: 25.01 μM

PKA,EGFR {[allProObj[0].p_purity_real_show]}
Dequalinium Chloride {[allProObj[0].p_purity_real_show]}
Quercetin Src,Sirtuin {[allProObj[0].p_purity_real_show]}
Myricetrin {[allProObj[0].p_purity_real_show]}
Go 6983 +++

PKCα, IC50: 7 nM

+++

PKCβ, IC50: 7 nM

+++

PKCγ, IC50: 6 nM

+++

PKCδ, IC50: 10 nM

++

PKCζ, IC50: 60 nM

{[allProObj[0].p_purity_real_show]}
Go6976 +++

PKC, IC50: 7.9 nM

++++

PKCα, IC50: 2.3 nM

+++

PKCβ1, IC50: 6.2 nM

FLT3 {[allProObj[0].p_purity_real_show]}
Bisindolylmaleimide I +++

PKCα, IC50: 20 nM

+++

PKCβ2, IC50: 16 nM

PKCβ1, IC50: 17 nM

+++

PKCγ, IC50: 20 nM

{[allProObj[0].p_purity_real_show]}
Lawsone methyl ether {[allProObj[0].p_purity_real_show]}
Sotrastaurin ++++

PKCα, Ki: 0.95 nM

++++

PKCβ1, Ki: 0.64 nM

++++

PKCδ, Ki: 2.1 nM

++++

PKCε, Ki: 3.2 nM

++++

PKCη, Ki: 1.8 nM

++++

PKCθ, Ki: 0.22 nM

{[allProObj[0].p_purity_real_show]}
Enzastaurin ++

PKCα, IC50: 39 nM

+++

PKCβ, IC50: 6 nM

+

PKCγ, IC50: 83 nM

+

PKCε, IC50: 110 nM

{[allProObj[0].p_purity_real_show]}
Midostaurin ++

PKCα, IC50: 22 nM

++

PKCβ2, IC50: 31 nM

PKCβ1, IC50: 30 nM

++

PKCγ, IC50: 24 nM

+

PKCδ, IC50: 330 nM

+

PKCε, IC50: 1.25 μM

+

PKCη, IC50: 160 nM

{[allProObj[0].p_purity_real_show]}
Ro 31-8220 mesylate ++++

PKCα, IC50: 5 nM

+++

PKCβ2, IC50: 14 nM

PKCβ1, IC50: 24 nM

++

PKCγ, IC50: 27 nM

++

PKCε, IC50: 24 nM

{[allProObj[0].p_purity_real_show]}
Staurosporine ++++

PKCα, IC50: 2 nM

++++

PKCγ, IC50: 5 nM

+++

PKCδ, IC50: 20 nM

++

PKCε, IC50: 73 nM

++++

PKCη, IC50: 4 nM

{[allProObj[0].p_purity_real_show]}
Ruboxistaurin HCl +

PKCα, IC50: 0.36 μM

++++

PKCβ2, IC50: 5.9 nM

PKCβ1, IC50: 4.7 nM

+

PKCγ, IC50: 0.3 μM

+

PKCδ, IC50: 0.25 μM

++

PKCη, IC50: 0.052 μM

{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 ALK1 ALK2 ALK3 ALK4 ALK6 Smad3 TGF-β TGFβRI/ALK5 TGFβRII 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

{[allProObj[0].p_purity_real_show]}
LDN-212854 ++++

ALK1, IC50: 2.4 nM

++++

ALK2, IC50: 1.3 nM

+

ALK3, IC50: 85.8 nM

+

ALK4, IC50: 2133 nM

+

ALK5, IC50: 9276 nM

{[allProObj[0].p_purity_real_show]}
ML347 ++

ALK1, IC50: 46 nM

++

ALK2, IC50: 32 nM

{[allProObj[0].p_purity_real_show]}
K02288 ++++

ALK1, IC50: 1.8 nM

++++

ALK2, IC50: 1.1 nM

++

ALK3, IC50: 34.4 nM

+++

ALK6, IC50: 6.4 nM

{[allProObj[0].p_purity_real_show]}
LDN-193189 dihydrochloride ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

{[allProObj[0].p_purity_real_show]}
LDN-214117 ++

ALK2, IC50: 24 nM

{[allProObj[0].p_purity_real_show]}
DMH-1 +

ALK2, IC50: 107.9 nM

{[allProObj[0].p_purity_real_show]}
SB-505124 +

ALK4, IC50: 129 nM

++

ALK5, IC50: 47 nM

{[allProObj[0].p_purity_real_show]}
Vactosertib +++

ALK4, IC50: 13 nM

+++

ALK5, IC50: 11 nM

{[allProObj[0].p_purity_real_show]}
Alantolactone {[allProObj[0].p_purity_real_show]}
SIS3 {[allProObj[0].p_purity_real_show]}
Pirfenidone {[allProObj[0].p_purity_real_show]}
Hesperetin {[allProObj[0].p_purity_real_show]}
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

{[allProObj[0].p_purity_real_show]}
GW788388 +++

ALK5, IC50: 18 nM

{[allProObj[0].p_purity_real_show]}
LY364947 ++

TGFβRI, IC50: 59 nM

+

TGFβRII, IC50: 0.4 μM

{[allProObj[0].p_purity_real_show]}
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

{[allProObj[0].p_purity_real_show]}
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

{[allProObj[0].p_purity_real_show]}
LY2109761 ++

TβRI, Ki: 38 nM

+

TβRII, Ki: 300 nM

{[allProObj[0].p_purity_real_show]}
Galunisertib ++

TβRI, IC50: 56 nM

{[allProObj[0].p_purity_real_show]}
SB 431542 +

ALK5, IC50: 94 nM

{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Aurothiomalate sodium 生物活性

描述 Aurothiomalate sodium is a potent and selective inhibitor of oncogenic PKCι signalling. Aurothiomalate sodium inhibits tumour cell proliferation but not apoptosis. Aurothiomalate sodium is a potent inhibitor of TrxR. Aurothiomalate sodium is an antirheumatic drug with strong antitumour activity[1][2][3].At concentrations of 0.001, 0.01, 0.1, 1, 10, 100, and 1000 uM, Aurothiomalate sodium induced inhibition of anchorage-independent growth in a dose-dependent manner in subject cell lines with IC50 of 300 nM-107 µM. Aurothiomalate sodium can induce inhibition of anchorage-independent growth in a dose-dependent manner with an IC50 of 300 nM-107 µM, including the A549, H1437, H2170, H460, H510, H187, H1703, and A427 lung cancer cell lines. Lung adenocarcinoma (LAC) and small cell lung cancer (SCLC) cells were more sensitive to Aurothiomalate sodium, while lung adenocarcinoma (LAC) was less sensitive to Aurothiomalate sodium. Aurothiomalate sodium blocked PKCι-Par6- by binding PKCι Rac1-Pak-Mek 1,2-Erk 1,2 signalling pathway activation and inhibits the growth of non-small lung cancer (NSCLC)[1].Aurothiomalate sodium inhibits TNFα-induced NF-kB activation and the expression of NF-kB-targeted pro-inflammatory genes (e.g., E-selectin and COX-2) at a concentration of 25 uM for 6 hours[3].

Aurothiomalate sodium 动物研究

Animal study Aurothiomalate sodium administered intramuscularly at doses of 2, 6, 20 or 60 mg/kg/day for 40 days had a statistically significant inhibitory effect on tumour growth in A427 cell tumours at all concentrations tested as A427 cells showing highly response[1].At 20 and 60 mg/kg/day, administered intramuscularly for 15 days, Aurothiomalate sodium showed statistically significant inhibition of H460 tumours only at the 60 mg/kg dose because of the low response of H460 cells[1].Aurothiomalate sodium reduced tumour growth in three-week-old KrasLA2 mice when administered intraperitoneally at a dose of 60 mg/kg/day for six weeks. Aurothiomalate sodium inhibited Kras-mediated expansion of bronchioalveolar stem cells (BASCs) and lung tumourigenesis in vivo[2].

Aurothiomalate sodium 参考文献

[1]Roderick P Regala, 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.

[2]Roderick P Regala, 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]Atsuko Sakurai, et al. Overexpression of thioredoxin reductase 1 regulates NF-kappa B activation. J Cell Physiol. 2004 Jan;198(1):22-30.

Aurothiomalate sodium 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.51mL

2.70mL

1.35mL

27.02mL

5.40mL

2.70mL

Aurothiomalate sodium 技术信息

CAS号12244-57-4
分子式C4H6AuNaO4S
分子量 370.109
别名 金硫丁二酸钠
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

H2O: 250 mg/mL(675.48 mM),配合低频超声助溶

动物实验配方
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