TRi-1 (TXNRD1 inhibitor 1)

Chemical Structure : TRi-1

CAS No.: 246020-68-8

Catalog No.: PC-63164Not For Human Use, Lab Use Only.

TRi-1 (TXNRD1 inhibitor 1) is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1) with anticancer potential, 5- to 10-fold higher specificity for TXNRD1 over TXNRD2.

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5 mg	$98	In stock
10 mg	$148	In stock
25 mg	$258	In stock
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Biological Activity

TRi-1 (TXNRD1 inhibitor 1) is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1, TrxR1) with anticancer potential, 5- to 10-fold higher specificity for TXNRD1 over TXNRD2.

TRi-1 block STAT3-dependent transcriptional activity with IC50 of 2.9 uM in in IL6-STAT3 luciferase reporter assays, 8-fold selectivity over IFN-γ STAT1.

TRi-1 inhibits cellular TXNRD activity with equal or greater potency compared to that of Auranofin with no effect on cellular GSH concentrations, efficiently activates c-Jun N-terminal kinase (JNK) and p38 phosphorylation.

TRi-1 shows cytotoxicity profile against the NCI-60 cell panel with mean IC50 of 6.41 uM.

TRi-1 impairs growth and viability of human tumor xenografts and syngeneic mouse tumors while having little mitochondrial toxicity and being better tolerated than auranofin.

Physicochemical Properties

M.Wt	328.723
Formula	C12H9ClN2O5S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-((4-chlorophenyl)sulfonyl)-6-methoxy-3-nitropyridine

References

1. Stafford WC, et al. Sci Transl Med. 2018 Feb 14;10(428). pii: eaaf7444.
2. S Busker, et al. Sci Adv. 2020 Mar 20;6(12):eaax7945.