TrxR Inhibitor, D9

A cell permeable, highly stable phosphinyl gold (I) acetylide complex that acts as a highly potent inhibitor of thioredoxin reductase (TrxR; EC₅₀ = 2.8 nM). Acts by blocking the redox-active selenenylsulfide motif of TrxR in an irreversible manner. Displays high selectivity over glutathione reductase (EC₅₀ >1000 nM). Selectively reduces the viability and proliferation of MCF-7 and HT-29 cancer cells (IC₅₀ = 30 and 100 nM, respectively) without affecting normal cells. Suppresses the growth of MCF-7 xenografts in BALB/c nude mice (5 mg/kg; i.v.,given on alternate days for 15 days).

A cell permeable, highly stable phosphinyl gold (I) acetylide complex that acts as a highly potent inhibitor of thioredoxin reductase (TrxR; EC₅₀ = 2.8 nM). Acts by blocking the redox-active selenenylsulfide motif of TrxR in an irreversible manner. Displays high selectivity over glutathione reductase (EC₅₀ >1000 nM). Selectively reduces the viability and proliferation of MCF-7 and HT-29 cancer cells (IC₅₀ = 30 and 100 nM, respectively) without affecting normal cells. Suppresses the growth of MCF-7 xenografts in BALB/c nude mice (5 mg/kg; i.v.,given on alternate days for 15 days).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

TrxR Inhibitor, D9, is a cell permeable, highly stable phosphinyl gold (I) acetylide complex that acts as a highly potent inhibitor of thioredoxin reductase (TrxR; EC₅₀ = 2.8 nM).

Cell permeable: yes

Primary Target
TrxR

Reversible: no

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Zhang, D., et al. 2014. J. Med. Chem.57, 8132.

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