TRi-1

• CAT Number: I019160
• CAS Number: 246020-68-8
• Molecular Formula: C12H9ClN2O5S
• Molecular Weight: 328.73
• Purity: ≥95%
• Synonyms: 2-(4-chlorophenyl)sulfonyl-6-methoxy-3-nitropyridine
• InChI: InChI=1S/C12H9ClN2O5S/c1-20-11-7-6-10(15(16)17)12(14-11)21(18,19)9-4-2-8(13)3-5-9/h2-7H,1H3
• InChIKey: PRKWNRUVAZZHPH-UHFFFAOYSA-N
• SMILES: COC1=NC(=C(C=C1)[N+](=O)[O-])S(=O)(=O)C2=CC=C(C=C2)Cl

TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy[1].
TRi-1 (0.679 and 6.79 μM; 6 h) has no effect on cellular glutathione (GSH) concentrations in FaDu cells, efficiently activates JNK and p38 phosphorylation[1].?
TRi-1 (2 μM) irreversibly inhibit TXNRD1 in an NADPH-dependent manner[1].?
TRi-1 (0.1-10 μM; 0-10 h) increases cellular H2O2 production in cultured FaDu cells in a concentration- and time-dependent manner[1].?
TRi-1 (10 nM-100 μM; 48 h) shows cytotoxicity toward cancer cells[1].
TRi-1 (10 mg/kg; i.v.; twice a day for 4 days or 5 mg/kg; i.p.; twice a week for 3 weeks) impaires growth and viability of human tumor xenografts and syngeneic mouse tumors[1].

Reference

[1]. Stafford WC, et al. Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy. Sci Transl Med. 2018 Feb 14;10(428). pii: eaaf7444.
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