TrxR Inhibitor

ROS-generating agent 1 is a selective ROS-generating agent. ROS-generating agent 1 inhibits TrxR activity and expression in cancer cells. ROS-generating agent 1 induces ROS-dependent apoptosis and ferroptosis in cancer cells. ROS-generating agent 1 selectively kills lung cancer cells and inhibits the growth of cancer cell xenograft tumors in nude mice. ROS-generating agent 1 can be used for the research of non-small cell lung cancer.

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.

Necroptosis inducer 1 is a necroptosis inducer. Necroptosis inducer 1 inhibits the activity of thioredoxin reductase (TrxR), elevates intracellular ROS levels, triggers ROS-mediated necroptosis, and induces necroptosis-dependent immunogenic cell death. Necroptosis inducer 1 inhibits tumor growth, remodels the tumor immune microenvironment, and exerts a synergistic effect with anti-PD-1 in animal models. Necroptosis inducer 1 is applicable to the research of colon cancer.

TrxR-IN-9 is a thioredoxin reductase (TrxR) inhibitor with an IC₅₀ of 0.26 μM. TrxR-IN-9 disrupts cellular redox balance. TrxR-IN-9 induces S-phase cell cycle arrest, promotes apoptosis and exhibits antiproliferative activity across cancer cells. TrxR-IN-9 exerts effects via synergistic nitric oxide (NO) and reactive oxygen species (ROS) action. TrxR-IN-9 can be used for the research of breast cancer, gastric cancer, colorectal cancer, liver cancer.

TrxR-IN-2 is a thioredoxin reductase (TrxR) inhibitor. TrxR-IN-2 increases reactive oxidative species (ROS) levels and decreases mitochondrial transmembrane potential levels. TrxR-IN-2 triggers DNA damage via H2AX regulation, and induces autophagy via LC3, beclin-1, and p62 regulation. TrxR-IN-2 can be used for the research of drug-resistant hepatocellular carcinoma^[1].

Nitrovin (Difurazon) is a thioredoxin reductase 1 (TrxR1) inhibitor with both antibacterial and anticancer activities. Nitrovin interacts with TrxR1 to generate reactive oxygen species (ROS), which in turn induces cytoplasmic vacuolization, activates MAPK and inhibits Alix. Nitrovin induces paraptosis-like non-apoptotic cell death, thereby exerting significant cytotoxicity against cancer cells. Nitrovin can be used in the research of heart disease and glioblastoma multiforme.

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.

As-CA11 is a Thioredoxin reductase (TrxR) inhibitor with an IC₅₀ of 18.7 nM. As-CA11 can induce cancer cells apoptosis and ROS production. As-CA11 can reduce the level of reduced Trx and increase the level of oxidized Trx. As-CA11 demonstrates anti-tumor activity in the 4T1 tumor-bearing mouse model.

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.

CS47 is a Thioredoxin Reductase 1 (TRXR1) inhibitor and ferroptosis inducer. CS47 binds non-covalently to sites between the FAD and NADPH pockets of TRXR1. CS47 drives glutathione depletion, lipid reactive oxygen species accumulation, HMOX1-dependent iron overload, and selective cytotoxicity in lung cancer cells. CS47 can be used for the research of 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.

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 (Compound L1Au2) is a TrxR/EGFR inhibitor. TrxR/EGFR-IN-1 is active against both Gefitinib (HY-50895)-sensitive and resistant lung cancers, effectively inhibiting tumor proliferation and promoting apoptosis. TrxR/EGFR-IN-1 promotes the degradation of GPX4 protein through autophagolysosomal and proteasomal pathways, leading to ferroptosis. In addition, TrxR/EGFR-IN-1 can induce endoplasmic reticulum stress and trigger immunogenic cell death. TrxR/EGFR-IN-1 can be used for the research of Gefitinib (HY-50895)-resistant lung cancer.

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.