TRi-1

SKU: orb1301755

Description

TRi-1 is a potent and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), exhibiting an IC50 of 12 nM. It demonstrates minimal mitochondrial off-target effects, making it a promising chemical probe for anticancer research in both cellular and animal models to investigate redox biology and therapeutic strategies.

Research Area

Signal Transduction

Key Properties

• CAS Number: 246020-68-8
• MW: 328.73
• Purity: 98.40% (May vary between batches)
• Formula: C₁₂H₉ClN₂O₅S
• SMILES: COc1ccc(c(n1)S(=O)(=O)c1ccc(Cl)cc1)[N+]([O-])=O
• Target: p38 MAPK,JNK,Others
• Solubility: DMSO:62.5 mg/mL (190.13 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.08 mM)

Bioactivity

• Target IC50:
  TXNRD1:12 nM
• In Vivo:
  The anticancer efficacy of TRi-1 in mouse tumor models is consistent with the idea that TXNRD1 is important for cancer cell growth in vivo
• In Vitro:
  TRi-1, impaired growth and viability of human tumor xenografts and syngeneic mouse tumors while having little mitochondrial toxicity and being better tolerated than auranofin.
• Animal Research:
  Fox Chase male SCID mice were treated once with TRi-1 (0.7 to 10 mg/kg) or TRi-2 (0.5 to 20 mg/kg) via intravenous injections, and mouse health status was observed for up to 72 hours. For repeateddose toxicity studies with tumor-bearing animals, mice were first inoculated with 1*10^6 FaDu cells in phosphate-buffered saline at a preshaved region located at the anterior lateral thoracic wall . After 13 days of growth, tumors were measured by calipers, and treatments were initiated. Mice were injected with TRi-1 (10 mg/kg), TRi-2 (15 mg/kg), auranofin (10 mg/kg), or vehicle a total of nine times during a 5-day span via intravenous tail injection. Upon the final day of dosing, injections were performed subcutaneously due to hematomas in several of the mice at the tail injection site. Mouse health status was monitored daily, weight was measured, and tumor volume was recorded from caliper measurements.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TXNRD1, TRi 1, TRi1, TRi-1, thioredoxin reductase 1, glutathione, FaDu, Inhibitor, inhibit, antitumor, cytosolic thioredoxin reductase 1 (TXNRD1)

Compound Identifiers

PubChem CID

2801235