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抑制剂描述:

产品名称:Auranofin

产品别名:见爱必信官网

英文别名:Auranofin

靶点:DUB

CAS:34031-32-8

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Auranofin is an inhibitor of thioredoxin reductase (TrxR) (IC50 = 20 nM; Ki = 4 nM for the NADPH-reduced form of human cytosolic TrxR). Auranofin induced the mitochondrial permeability transition via inhibition of mitochondrial TrxR. Auranofin also exhibits anti-inflammatory and immunosuppressive activities. Auranofin inhibits 5-lipoxygenase at high concentrations and stimulates LTA hydrolase at low concentrations.

溶解性:DMSO : ≥5mg/mL

体外研究:

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. 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. 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.

体内研究: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.

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