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).
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).
Biochem/physiol Actions
Cell permeable: yes
Primary Target TrxR
Reversible: no
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Zhang, D., et al. 2014. J. Med. Chem.57, 8132.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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