trxr-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.

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.

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].

TP-TRFS is a highly selective and the first two-photon fluorescent probe of thioredoxin reductase (TrxR) [1] .

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].

S-Gem, a thioredoxin reductase (TrxR)-dependent prodrug of Gemcitabine, is selectively activated by TrxR. Studies indicate that S-Gem exhibits lower cytotoxicity than Gemcitabine [1].

TRFS-green, a highly selective off-on fluorescent probe, is designed for the specific imaging of thioredoxin reductase (TrxR) in living cells, exhibiting its maximum absorbance at approximately 373 nm [1].

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].

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].

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.

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.