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Aurothiomalate sodium

CAS No. : 12244-57-4

MCE 国际站：Aurothiomalate sodium

产品活性：Aurothiomalate sodium 是一种有效的和选择性的致癌 PKC_ι 信号传导抑制剂。Aurothiomalate sodium 抑制肿瘤细胞增殖，而不抑制细胞凋亡。Aurothiomalate sodium 是一种有效的硫氧还蛋白还原酶 (TrxR) 抑制剂。Aurothiomalate sodium 是一种抗风湿剂，显示出有效的抗肿瘤活性。

研究领域：Epigenetics  |  TGF-beta/Smad

作用靶点：PKC

In Vitro: Aurothiomalate sodium (0.001, 0.01, 0.1, 1, 10, 100, 1000 uM) induces dose-dependent inhibition of anchorage-independent growth in all cell lines tested (A549, H1437, H2170, H460, H510, H187, H1703 and A427 lung cancer cell lines) with IC₅₀s ranging from 300 nM-107 µM. The lung adenocarcinoma (LAC) and small cell lung carcinoma (SCLC) cells tends to be more sensitive and lung adenocarcinomas (LACs) less sensitive to Aurothiomalate sodium.
Aurothiomalate sodium (25 uM; 6 hours) suppresses TNFa-induced activation of NF-kB and the expression of NF-kB-targeted proinflammatory genes such as E-selectin and cyclooxygenase-2.
Aurothiomalate sodium inhibits non-small lung cancer (NSCLC) growth by binding PKC_ι and blocking activation of a PKC_ι-Par6-Rac1-Pak-Mek 1,2-Erk 1,2 signaling pathway.
Aurothiomalate sodium inhibits Mek/Erk signaling and decreases proliferative index without effecting tumor apoptosis or vascularization in vivo.

In Vivo: Aurothiomalate sodium (2, 6, 20 or 60 mg/kg/day; intramuscular injections; 40 days) exhibits statistically significant inhibition of tumor growth at all concentrations tested in A427 cell tumors because A427 cells are highly responsive.
Aurothiomalate sodium (20, 60 mg/kg/day; intramuscular injections; 15 days) shows a statistically significant response (~50% reduction in tumor size) only at the 60 mg/kg dose in H460 tumors because H460 cells are less responsive.
Aurothiomalate sodium (60 mg/kg/day; IP; for six weeks) exhibites a decrease in tumor growth in Three-week-old KrasLA2 mice. Aurothiomalate sodium inhibits Kras-mediated bronchioalveolar stem cells (BASCs) expansion and lung tumorigenesis in vivo.

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