5.32910

TrxR Inhibitor, D9

• Synonym(s): TrxR Inhibitor, D9, Thioredoxin inhibitor, D9
• Empirical Formula (Hill Notation): C₂₅H₂₀AuOPS
• Molecular Weight: 596.43
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mg/mL
• storage temp.: −20°C

Description

General description

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).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
TrxR

Reversible: no

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable