TrxR Inhibitor

Aurothiomalate disodium acts as an inhibitor of PKCI and TrxR1. Aurothiomalate disodium disrupts the PKCI-Par6-Rac1 signaling pathway, and also inhibits TrxR1 activity, TNFα-induced NF-κB activation, and the expression of pro-inflammatory genes. Aurothiomalate disodium blocks Kras-mediated BASC expansion and lung tumor growth, inhibits anchorage-independent growth and tumorigenicity of lung cancer cells, and suppresses neutrophil chemotaxis, phagocytosis, and leukocyte extravasation. Aurothiomalate disodium can be used in research related to rheumatoid arthritis and non-small cell lung cancer.

TrxR-IN-6 is a thioredoxin reductase (TrxR) inhibitor. TrxR-IN-6 induces reactive oxygen species (ROS) accumulation and cell apoptosis. TrxR-IN-6 induces mitochondrial dysfunction, endoplasmic reticulum stress and DNA damage. TrxR-IN-6 can be used for the research of breast cancer, leukemia.

TrxR-IN-4 is a thioredoxin reductase (TrxR) inhibitor with a rat IC₅₀ of 0.37 μM. TrxR-IN-4 inhibits TrxR activity, elevates reactive oxygen species (ROS) and induces apoptosis. TrxR-IN-4 mediates endoplasmic reticulum stress and induces mitochondrial dysfunction. TrxR-IN-4 can be used for the research of hepatocellular carcinoma.

Platinum (IV) Prodrug-1 is a Pt (IV) prodrug and selective TrxR1 inhibitor. Platinum (IV) Prodrug-1 induces ferroptosis (Ferroptosis) by depleting glutathione, accumulating intracellular lipid peroxides, and inactivating Glutathione peroxidase 4. Platinum (IV) Prodrug-1 triggers endoplasmic reticulum stress and immunogenic cell death via excessive accumulation of intracellular ROS. Platinum (IV) Prodrug-1 exhibits anticancer activity against both Cisplatin (HY-17394)-sensitive and Cisplatin-resistant triple-negative breast cancer cells. Platinum (IV) Prodrug-1 can be used for the research of triple-negative breast cancer.

TrxR-IN-7 is a thioredoxin reductase (TrxR) inhibitor with an IC₅₀ of 3.5 μM. TrxR-IN-7 induces reactive oxygen species (ROS) generation and apoptosis in tumor cells. TrxR-IN-7 can be used for the research of liver cancer and breast cancer.

TrxR1-IN-2 (Compound 6a) is a TrxR1 inhibitor that covalently binds to the Cys475 and Sec498 sites of TrxR1, thereby inhibiting TrxR1 activity and leading to redox homeostasis disruption, which triggers apoptosis and ferroptosis.

LW-216 is a TrxR1 inhibitor that induces Apoptosis. LW-216 has anti-tumor activity.

FEACYP is a thioredoxin reductase (TrxR) inhibitor. FEACYP inhibits thioredoxin reductase activity, induces ROS by increasing basal cellular hydrogen peroxide production, suppresses tumor growth, exerts cytotoxicity against human cancer cells, and exhibits antiproliferative activity in human pancreatic cancer 3D spheroids. FEACYP can be used in the research of ovarian cancer, colon cancer, pancreatic cancer, and lung cancer.

TrxR/EGFR-IN-1 is a TrxR/GFR inhibitor and a Gefitinib (HY-50895) derivative. TrxR/EGFR-IN-1 inhibits TrxR and EGFR, downregulates p‑EGFR, p‑AKT, and p‑ERK; promotes GPX4 protein degradation through dual autophagy-lysosomal and proteasomal pathways, triggering ferroptosis. TrxR/EGFR-IN-1 induces endoplasmic reticulum stress, immunogenic cell death, and apoptosis, increasing intracellular ROS and oxidative stress. TrxR/EGFR-IN-1 exhibits in vitro antiproliferative activity against both Gefitinib-sensitive and Gefitinib-resistant non-small cell lung cancer. TrxR/EGFR-IN-1 inhibits tumor growth in the PC9GR xenograft tumor model. TrxR/EGFR-IN-1 can be used for lung cancer-related research.

TrxR2-IN-1 is a thioredoxin reductase 2 (TrxR2) inhibitor with an IC₅₀ value of 0.83 μM. TrxR2-IN-1 accumulates in mitochondria, impairs mitochondrial function and membrane potential, increases reactive oxygen species (ROS) levels, activates ASK1-mediated caspase-dependent apoptosis (apoptosis), induces G2/M cell cycle arrest, and inhibits cancer cell migration. TrxR2-IN-1 can be used in the research of hepatocellular carcinoma.

TrxR-IN-8 (Compound 6f) is a selective TrxR inhibitor (IC₅₀: 10.2 μM). TrxR-IN-8 induces apoptosis through oxidative stress by stimulating the production of reactive oxygen species (ROS), reducing intracellular thiols, and lowering the glutathione/glutathione ratio. TrxR-IN-8 exhibits significant cytotoxicity against non-small cell lung cancer (NSCLC) cells.

Photosensitizer-6 (Compound 4) is a gold (I) complex and exhibits inhibitory activity against TrxR. Photosensitizer-6 induces apoptosis in 4T1 cell, targets and eradicates tumors through chemo-phototherapy and immunogenic cell death under light exposure. Photosensitizer-6 can be used for tumor imaging.

DDHF20 is an antimicrobial agent against Staphylococcus aureus, targeting and inhibiting its thioredoxin reductase (TrxR). It acts as a competitive inhibitor for the NADPH binding site. DDHF20 is expected to be used in research related to antimicrobial infections caused by Staphylococcus aureus.

MMV085203 is a potent Plasmodium falciparum inhibitor, with a PfTrxR EC₅₀ of 900 nM. MMV085203 exerts potent antimalarial activity against both blood‑stage and sexual‑stage Plasmodium falciparum parasites, with superior efficacy toward clinical isolates of high clonal diversity. MMV085203 modulates parasite redox homeostasis, induces ROS production, and elevates mitochondrial TCA cycle intermediates. MMV085203 can be used for the research of malaria.

PAO-PDT is an organoarsenic inhibitor of thioredoxin reductase (TrxR), with an IC₅₀ of 33 nM. PAO-PDT can bind to the C-terminal selenocysteine/cysteine pair of TrxR and convert the enzyme into an NADPH oxidase, which increases reactive oxygen species levels and impairs mitochondrial respiratory function, thereby inducing apoptosis in leukemia cells. PAO-PDT can be used for leukemia research.