trxr

Auranofin (SKF-39162) is an antirheumatic agent, is used to treat rheumatoid arthritis, improves arthritis symptoms including painful or tender and swollen joints and morning stiffness.

TrxR-IN-7 (14f) is a potent inhibitor of thioredoxin reductase (TrxR), with an IC50 value of 3.5 µM. It exhibits antiproliferative activity and can induce apoptosis and the production of reactive oxygen species (ROS).

TrxR EGFR-IN-1 (Compound L1Au2) is a TrxR EGFR inhibitor with activity against both gefitinib-sensitive and -resistant lung cancer, effectively suppressing tumor proliferation and promoting apoptosis. It enhances GPX4 degradation through autophagosome-lysosome and proteasome pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it applicable for studies on gefitinib-resistant lung cancer.

TrxR-IN-D9 is a novel inhibitor of thioredoxin reductase (TrxR).

TrxR-IN-3 (Compound 2c) is an effective TrxR inhibitor that exhibits strong antiproliferative activities against five human cancer cell lines, particularly breast tumor cells. It increases ROS levels, induces apoptosis by regulating apoptosis-related protein expression in breast cancer cells, and promotes autophagosome and autolysosome formation by enhancing LC3-II and Beclin-1 expression and reducing LC3-I and p62 protein expression [1].

TrxR-IN-5 (compound 4f) is an efficacious inhibitor of TrxR (thioredoxin reductase) with an IC50 of 0.16 μM. By elevating the levels of reactive oxygen species (ROS), TrxR-IN-5 fosters robust antiproliferative impacts and demonstrates pronounced effects against cancer proliferation and metastasis [1].

TrxR-IN-2 is a potential thioredoxin reductase (TrxR) inhibitor. TrxR-IN-2 has research value in the chemotherapy of drug-resistant hepatocellular carcinoma.

Compound 1b (TrxR-IN-4) is a potent TrxR inhibitor that activates endoplasmic reticulum stress (ERS) to induce apoptosis in HepG2 cells and mitigates CCl4-induced liver damage in vivo through TrxR expression down-regulation and reduced inflammation [1].

TrxR1-IN-B19 (TrxR1 IN B19), a TrxR1 inhibitor, selectively kills gastric cancer cells by a small molecule via targeting TrxR1 and ROS-mediated ER stress activation.

TrxR1 prodrug-1 (compound 5u) is a potent inhibitor of TrxR1, demonstrating significant antitumor activity in nude mice and NSCLC organoids.

TrxR1-IN-2 (Compound 6a) acts as a TrxR1 inhibitor that covalently bonds with the Cys475 and Sec498 sites of TrxR1. This interaction hampers TrxR1 activity, resulting in a redox homeostasis disruption and inducing apoptosis and ferroptosis.

Compound 5j, also known as TrxR1-IN-1, is a TrxR1 inhibitor with an IC50 of 8.8 μM. It exhibits anticancer activity, demonstrating IC50 values of 1.5 μM in MCF-7, 1.7 μM in HeLa, 2.4 μM in BGC-823, 2.8 μM in SW-480, and 2.1 μM in A549 cells. Additionally, TrxR1-IN-1 possesses antioxidant activity, effectively scavenging the DPPH radical [1].

Ethaselen (BBSKE) is an orally active and selective thioredoxin reductase 1 (TrxR) inhibitor with anticancer activity that directly inhibits TrxR1 activity and is commonly used in combination with oxaliplatin to inhibit tumor growth.Ethaselen induces apoptosis in cancer cells and inhibits the proliferation of colorectal cancer cells.

Ros-generating agent 1 has anticancer activity and generates ROS by covalently modifying Sec-498 residues of TrxR. ROS-generating agent 1 reduces intracellular TrxR protein levels and promotes ROs-dependent apoptosis and ferroptosis in NCI-H460 cells.

Manumycin A is an antibiotic with anticancer activity and is a mammalian thioredoxin reductase-1 (TrxR-1) inhibitor.Manumycin A inhibits the production of IL-1β, IL-6, and IL-8 in TNF alpha-stimulated THP-1 cells and peripheral blood mononuclear cells in a dose-dependent manner, inducing apoptosis.

Photosensitizer-6 (Compound 4) is a metal ion complex that inhibits TrxR. It induces apoptosis in 4T1 cells, targeting cancer cells and eliminating tumors through chemophototherapy and immunogenic cell death under illumination. Additionally, Photosensitizer-6 can be utilized for tumor imaging.

[Au(L4)(CyJohnPhos)]SbF6 is a gold-containing compound that exhibits inhibitory effects on cyclooxygenase-1 2 (COX-1 2), suppresses the proliferation of colon cancer cells Caco2- TC7 with an IC50 of 0.98 μM, and induces cell apoptosis (apoptosis). Additionally, [Au(L4)(CyJohnPhos)]SbF6 acts as an inhibitor of thioredoxin reductase (TrxR) and demonstrates antioxidative activity by modulating ROS levels.

Sodium aurothiomalate is a gold compound that is used for its immunosuppressive anti-rheumatic effects. Aurothiomalate sodium (Miochrysin) is a potent and selective inhibitor of oncogenic PKC-ι signaling. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium exhibits potent anti-tumor activity.

DDHF20 is an inhibitor of Staphylococcus aureus, specifically targeting and inhibiting its thioredoxin reductase (TrxR) by acting as a competitive inhibitor at the NADPH binding site. DDHF20 shows potential for research in combating infections related to Staphylococcus aureus.

BGC4 is a gold(III) complex based on biphenyl. It inhibits human recombinant thioredoxin reductase (TrxR) with an IC50 of 10.7 μM, exhibits cytotoxicity with an IC50 of 5.4 μM in MDA-MB-231 cells, and induces apoptosis. Additionally, BGC4 demonstrates antitumor activity in mouse models.

inhibitor of the thioredoxin-thioredoxin reductase (Trx-TrxR) system

ZC0101 is a potent, orally active dual inhibitor of IDO1 (IC50 = 0.084 μM) and TrxR (IC50 = 7.98 μM), which effectively induces apoptosis and ROS accumulation in cancer cells [1].

TPP2a is a mitochondrial thioredoxin reductase (TrxR) inhibitor.

CPUL1, a TrxR inhibitor, exhibits proliferation-inhibitory and anti-metastatic effects on A549 cells by modulating epithelial-mesenchymal transition (EMT) through the induction of ROS-mediated ERK JNK signaling, achieved by inhibiting TrxR1 enzyme activity. The efficacy of CPUL1 is enhanced when used in conjunction with α-Lipoic Acid or Dithiodipropionic acid [1].