1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. TrxR

TrxR

Thioredoxin Reductase

TrxR (Thioredoxin Reductase) is a selenium-containing pyridine nucleotide-disulphide oxidoreductase. There are three isoforms of mammalian TrxRs: TrxR1 (TXRND1), TrxR2 (TXNRD2) and TrxR3 (TGR). TrxRs catalyze the NADPH-dependent reduction of the redox protein thioredoxin (Trx). TrxR is important in regulating the intracellular redox environment, cell growth and transformation, as well as the recycling of ascorbate from its oxidized form. Trx/TrxR system is associated with the cancers, metabolic syndrome, insulin resistance, and type 2 diabetes, as well as in hypertension and atherosclerosis[1][2].

TrxR Isoform Specific Products:

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-115640
    TRFS-green
    TRFS-green is a highly selective off−on fluorescent probe for imaging selenoprotein thioredoxin reductase (TrxR) in living cells. TRFS-green has the maximum absorbance at around 373 nm. After it is activated by TrxR, the maximum absorbance shifts to around 440 nm.
    TRFS-green
  • HY-116749
    Ethaselen
    ≥98.0%
    Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR.
    Ethaselen
  • HY-150228
    MitoCur-1
    MitoCur-1, a curcumin analogue, is an inhibitor of mitochondrial antioxidative thioredoxin reductase 2 (TrxR2). MitoCur-1 has electrophilic and mitochondrial-targeting properties. MitoCur-1 induces reactive oxygen species (ROS) generation, exerts specifically antitumor efficacy.
    MitoCur-1
  • HY-149265
    ROS-generating agent 1
    Inhibitor 99.57%
    ROS-generating agent 1 (Compound 2c) covalently modifies the Sec-498 residue of TrxR to generate ROS. ROS-generating agent 1 reduces intracellular TrxR protein level. ROS-generating agent 1 results in ROS-dependent apoptosis and ferroptosis of NCI-H460 cells. ROS-generating agent 1 has anti-cancer activities.
    ROS-generating agent 1
  • HY-126322
    DVD-445
    98.65%
    DVD-445 (Compound 7) is a potent peptidomimetic covalent thioredoxin reductase 1 (TrxR1) inhibitor with an IC50 of 0.60 μM for rat TrxR1. DVD-445 has good anticancer application.
    DVD-445
  • HY-168875
    TrxR1 prodrug-1
    Inhibitor
    TrxR1 prodrug-1 (compound 5u) is a potent inhibitor of TrxR1. TrxR1 prodrug-1 exhibits significant antitumor efficiency in nude mice and NSCLC organoids.
    TrxR1 prodrug-1
  • HY-172115
    BGC4
    Inhibitor
    BGC4 is a biphenyl-based gold(III) complex. BGC4 inhibits human recombinant thioredoxin reductase (TrxR) with an IC50 of 10.7 μM, exhibits cytotoxicity (IC50 for MDA-MB-231 is 5.4 μM), and induces apoptosis. BGC4 exhibits antitumor efficacy in mouse models.
    BGC4
  • HY-172086
    TrxR-IN-7
    Inhibitor
    TrxR-IN-7 (14f) is a potent thioredoxin reductase (TrxR) inhibitor with an IC50 value of 3.5 µM. TrxR-IN-7 shows antiproliferative activity. TrxR-IN-7 induces apoptosis and ROS generation.
    TrxR-IN-7
  • HY-154843
    C-Gem
    Control
    C-Gem is a control molecule of S-Gem (HY-154842). C-Gem is completely inactive under experimental conditions.
    C-Gem
  • HY-132972
    TrxR-IN-2
    TrxR-IN-2, a potential thioredoxin reductase (TrxR) inhibitor, represents a promising candidate drug for the chemoresearch of drug-resistant hepatocellular carcinoma.
    TrxR-IN-2
  • HY-138071
    8α-Tigloyloxyhirsutinolide 13-O-acetate
    Inhibitor
    8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo.
    8α-Tigloyloxyhirsutinolide 13-O-acetate
  • HY-108534
    PMX464
    PMX464 (AW 464), a thiol-reactive quinol, is the inhibitor of thioredoxin-thioredoxin reductase (Trx/TrxR) system. PMX464 can inhibit NF-κB-mediated proinflammatory activation of human type II alveolar epithelial cells.
    PMX464
  • HY-D1253
    TP-TRFS
    TP-TRFS is a highly selective and the first two-photon fluorescent probe of thioredoxin reductase (TrxR).
    TP-TRFS
  • HY-129751
    Nitrovin hydrochloride
    Inhibitor
    Nitrovin hydrochloride is an antibacterial growth promoter. Nitrovin hydrochloride induces ROS-mediated non-apoptotic and apoptotic-like cell death by targeting TrxR1. Nitrovin hydrochloride has anticancer activity, with IC50 values of 1.31-6.60 μM for tumor and normal cells.
    Nitrovin hydrochloride
  • HY-146307
    TrxR-IN-3
    TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins.
    TrxR-IN-3
  • HY-149390
    TrxR1-IN-1
    Inhibitor
    TrxR1-IN-1 (Compound 5j) is a TrxR1 inhibitor (IC50: 8.8 μM). TrxR1-IN-1 has anticancer activity, with IC50s of MCF-7 (1.5 μM), HeLa (1.7 μM), BGC-823 (2.4 μM), SW-480 (2.8 μM), A549 (2.1 μM). TrxR1-IN-1 has antioxidant activity, and scavenges DPPH radical.
    TrxR1-IN-1
  • HY-157158
    TrxR-IN-6
    Inhibitor
    TrxR-IN-6 (compound 1d) is a TrxR inhibitor that induces reactive oxygen species (ROS) accumulation and has anticancer activity. TrxR-IN-6 can further lead to redox system collapse, inducing mitochondrial dysfunction, endoplasmic reticulum (ER) stress, and DNA damage. Finally, it causes oxidative stress and induces apoptosis.
    TrxR-IN-6
  • HY-146350
    TrxR-IN-4
    Inhibitor
    TrxR-IN-4 (Compound 1b) is a potent inhibitor of TrxR. TrxR-IN-4 induces HepG2 cells apoptosis by activating the endoplasmic reticulum stress (ERS). TrxR-IN-4 improves the CCl4-induced liver damage in vivo by down-regulation of TrxR expression and inflammation level.
    TrxR-IN-4
  • HY-163724
    LW-216
    Inhibitor
    LW-216 is a TrxR1 inhibitor that induces Apoptosis. LW-216 has anti-tumor activity.
    LW-216
  • HY-151802
    CPUL1
    CPUL1 is a TrxR inhibitor, which shows proliferation-inhibitory and anti-metastatic activity against A549 cells. CPUL1 influences EMT (epithelial-mesenchymal transition) via inducing ROS-mediated ERK/JNK signaling by inhibiting TrxR1 enzyme activity. CPUL1 in combination with α-Lipoic Acid (HY-N0492) or Dithiodipropionic acid (HY-W014395) is more effective.
    CPUL1
Cat. No. Product Name / Synonyms Application Reactivity

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