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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-STAT-TRi-1
TRi-1

Chemical Structure : TRi-1

CAS No.: 246020-68-8

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TRi-1 (TXNRD1 inhibitor 1)

货号: 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 ￥1280 In stock
10 mg ￥1880 In stock
25 mg ￥2980 In stock
50 mg ￥4880 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: 98.8% Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 328.723
分子式 C12H9ClN2O5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-((4-chlorophenyl)sulfonyl)-6-methoxy-3-nitropyridine

参考文献

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.

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