TRi-1

SKU: orb1220933

Description

TRi-1 is irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1) with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy.

Key Properties

• CAS Number: 246020-68-8
• MW: 328.72
• Purity: >98% (HPLC)
• Formula: C₁₂H₉ClN₂O₅S
• SMILES: COc1ccc(c(n1)S(=O)(=O)c1ccc(Cl)cc1)[N+]([O-])=O
• Target: TXNRD1
• Solubility: DMSO:62.5 mg/mL (190.13 mM)

Bioactivity

• In Vivo:
  Animal model: SCID mice bearing established human FaDu cell xenografts. Dosage: 10 mg/kg. Administration: Intravenous injection, twice a day for 4 days. Result: Resulted in decreased tumor growth compared to vehicle controls within four days with no signs of overt toxicity or changes in mouse weight relative to vehicle control. Animal model: PyMT-MMTV mice that spontaneously develop malignant breast cancer tumors. Dosage: 5 mg/kg. Administration: Intraperitoneal injection, twice a week for 3 weeks. Result: Impaired tumor growth, significantly reduced tumor volumes.
• In Vitro:
  Western blot analysis. Cell line: FaDu cells. Concentration: 0.679 and 6.79 μM Incubation time: 6 h. Result: Efficiently activated JNK and p38 phosphorylation. Cell Cytotoxicity Assay Cell line: Leukemia, non-small cell lung, CNS, colon, melanoma, ovarian, renal, prostate and breast cancer cells. Concentration: 10 nM-100 μM. Incubation time: 48 h. Result: Displayed potency against every cell line tested, with an average growth inhibition to 50% (GI50) of 6.31 μM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

TXNRD1