Ferroptosis Inducer

EGFR/tubulin-IN-1 (Compound 26) is a dual-target inhibitor of EGFR and tubulin. EGFR/tubulin-IN-1 significantly reduces the levels of p-EGFR, p-AKT, and p-ERK in cells, disrupting the microtubule structure of the cells. EGFR/tubulin-IN-1 significantly inhibits the proliferation of H1975 cells and significantly blocks the cells in the G2/M phase. EGFR/tubulin-IN-1 induces the expression of autophagy markers LC3B-II and Beclin-1, while down-regulating the expression of p62. EGFR/tubulin-IN-1 induces ferroptosis, with increased ROS content and depletion of glutathione (GSH). EGFR/tubulin-IN-1 inhibits epithelial-mesenchymal transition (EMT) and tumor metastasis. EGFR/tubulin-IN-1 has a significant tumor-suppressing effect in the H1975 transplanted tumor nude mouse model. EGFR/tubulin-IN-1 can be used for the study of non-small cell lung cancer.

anti-TNBC agent-6 (compound pt-3) is a potent anti-TNBC agent. anti-TNBC agent-6 shows cytotoxic activity. anti-TNBC agent-6 induces autophagy and ferroptosis. anti-TNBC agent-6 enhances intracellular ROS accumulatio. anti-TNBC agent-6 shows anti tumor activity and has the potential for the research of breast cancer.

DefNEtTrp is a Fe dual chelator ligand, consisting of the Def and Trp moieties. DefNEtTrp exhibits potent and broad-spectrum antiproliferative and cell death behavior in cancer cell lines. DefNEtTrp induces both apoptosis and ferroptosis and has cytotoxicity with an IC₅₀ value of 0.77 μM.

GPX4 degrader-2 is a GPX4 molecular glue degrader and ferroptosis inducer. GPX4 degrader-2 suppresses GPX4 enzyme activity, promotes ubiquitination-dependent proteasomal degradation of GPX4 protein. GPX4 degrader-2 indues ferroptosis, increases lipid ROS and MDA levels, suppresses glutathione levels in cancer cells. GPX4 degrader-2 inhibits cancer cells proliferation and colony formation. GPX4 degrader-2 can be used for the research of colorectal cancer.

FGFR-IN-28 is a FGFR inhibitor with inhibitory activity against multiple subtypes of the FGFR family, with an IC₅₀ of 4.4 nM against FGFR4. FGFR-IN-28 inhibits kinase activity and phosphorylation processes, and blocks the downstream MAPK and AKT signaling pathways. FGFR-IN-28 induces cellular DNA damage, cell cycle arrest, apoptosis and ferroptosis, and reduces the adhesion, invasion and metastasis abilities of cancer cells. FGFR-IN-28 exhibits anti-tumor activity in in vitro experiments on colon cancer cells, and inhibits tumor growth in colon cancer xenograft models. FGFR-IN-28 can be used in colon cancer-related research.

Ferroptosis inducer-5 (compund 20a) is a ferroptosis inducer.

HDAC-IN-77 (HL-5s) is an HDAC inhibitor. HDAC-IN-77 can induce ferroptosis and inhibit the Nrf2/HO-1 signaling pathway. HDAC-IN-77 can be used in cancer research.

GPX4-IN-23 (Compound 3e) is a GPX4 inhibitor with an IC₅₀ of 0.27 μM. GPX4-IN-23 induces Ferroptosis by enhancing lipid peroxidation, ROS production, and intracellular GSH depletion. GPX4-IN-23 exhibits antiproliferative activity against central nervous system cancer cells. GPX4-IN-23 can be used in studies related to central nervous system cancers.

GPX4 degrader-1 (Compound RS-1) is a hydrophobic tagging (HyT)-mediated GPX4 degrader (DC₅₀: 8.9 nM in HT1080 cells) GPX4 degrader-1 induces GPX4 degradation. GPX4 degrader-1 induces Ferroptosis. GPX4 degrader-1 increases lipid ROS. GPX4 degrader-1 demonstrates potent antitumor efficacy in a murine mammary carcinoma model.

Antitumor agent-125 (compound 17A) is a novel platinum(IV) prodrug. Antitumor agent-125 can activate the mitochondrion-dependent apoptosis pathway. Antitumor agent-125 induces ferroptosis in HCT-116/OXA.

SB-T-101141 is a novel taxane. SB-T-101141 effectively induces a noncanonical ferroptosis to overcome Paclitaxel (HY-B0015) resistance of breast cancer. SB-T-101141 facilitates the production of iron and ferrous ions and ROS. SB-T-101141 stably binds to KHSRP to inhibit the iron-dependent expression of CISD1 related to iron homeostasis. SB-T-101141 synergistically enhances the iron-dependent activation of JNK and PERK pathways via KHSRP. SB-T-101141 suppresses breast tumor growth in MCF-7(PR)/MDA-MB-231(PR) or KHSRP knock-down MCF-7 xenograft mice model.

Antiproliferative agent-70 (compound 23) is a potent antiproliferative agent. Antiproliferative agent-70 shows antiproliferative activities and induces MMP depolarization. Antiproliferative agent-70 induces mitochondrial dysfunction. Antiproliferative agent-70 induces mitophagy and ferroptosis. Antiproliferative agent-70 increases the protein expression of PINK1, p-Parkin, p53 and p21. Antiproliferative agent-70 increases intracellular ROS levels. Antiproliferative agent-70 shows anticancer activity.

hDHODH-IN-15 (Compound H19) is an inhibitor for human dihydroguanylate dehydrogenase (hDHODH) with an IC₅₀ of 0.21 µM. hDHODH-IN-15 exhibits cytotoxicity in cancer cells NCI-H226, HCT-116, and MDA-MB-231, with IC₅₀ of 0.95-2.81 µM. hDHODH-IN-15 induces ferroptosis in HCT-116, and exhibits antitumor efficacy.

Autophagy-IN/Ferroptosis inducer-modulator-1 is a dual-functional molecule that acts as an Autophagy inhibitor and a Ferroptosis inducer. Autophagy-IN/Ferroptosis inducer-modulator-1 downregulates GPX4 expression, elevates ROS levels and reduces mitochondrial membrane potential. Autophagy-IN/Ferroptosis inducer-modulator-1 arrests the cell cycle of non-small cell lung cancer (NSCLC) cells, induces mild apoptosis and inhibits autophagy. Autophagy inhibition induced by Autophagy-IN/Ferroptosis inducer-modulator-1 acts upstream of ferroptosis to produce a synergistic effect. Autophagy-IN/Ferroptosis inducer-modulator-1 exhibits anti-tumor activity against both human tumor cells and zebrafish xenograft models. Autophagy-IN/Ferroptosis inducer-modulator-1 can be used for research related to non-small cell lung cancer.

Fa-Au is a TrxR inhibitor. Fa-Au downregulates GPX4, induces oxidative stress, mitochondria-associated ferroptosis (ferroptosis) and immunogenic cell death. Fa-Au induces ROS production in hepatoma cells. Fa-Au remodels the tumor immune microenvironment via M1 macrophage polarization, dendritic cell maturation, CD8+ T cell activation and reduction of regulatory T cells. Fa-Au induces an anti-tumor immune feedback loop through the IFNγ/STAT1/SLC7A11 axis. Fa-Au inhibits tumor growth. Fa-Au is applicable to hepatocellular carcinoma-related research.

Ferroptosis inducer-4 (Compound 5) is a ferroptosis (Ferroptosis) inducer with a structure featuring terminal double bonds introduced at the sn-2 position of phospholipids. Ferroptosis inducer-4 exhibits significant cytotoxicity towards HT-1080 cells, with an IC₅₀ of 18 μM. This cytotoxic mechanism involves the generation of lipid peroxides and oxidative damage to the cell membrane triggered by the terminal double bonds. Ferroptosis inducer-4 can be used for research on ferroptosis regulation.

Anticancer agent 199 (Compound G-4) induces apoptosis in triple negative breast cancer (TNBC) cells via the mitochondrial pathway through inhibiting EGFR, AKT and MAPK pathways. Anticancer agent 199 also induces Ferroptosis by down-regulating LCN2. Anticancer agent 199 inhibits TNBC cell viability and migration, and induces S phase cell cycle arrest. Anticancer agent 199 is a derivate of cyclin-dependent kinase inhibitor Rocovitine.

Antitumor agent-196 (Compound 6a (β, β, β)) is an artemisinin-based oligomer with anticancer activity, showing an IC₅₀ of 90 nM against MCF-7 breast cancer cells. Antitumor agent-196 promotes Apoptosis by regulating the Bax-caspase 3 signaling pathway, and induces Ferroptosis through the modulation of key signaling molecules, including GPX4. Antitumor agent-196 holds promising potential for further research in the field of cancer therapy.

GPX4-IN-7 (Compound 31), indirubin derivative, is a ferroptosis inducer for colon cancer. GPX4-IN-7 has strong antitumor activity against HCT-116 cells with an IC₅₀ value of 0.49 μM. GPX4-IN-7 can promote the degradation of GPX4, causing the accumulation of lipid ROS to induce ferroptosis.

Ferroptosis inducer-16 (anti-NSCLC agent-2) is a nitric oxide (NO) donor and a ferroptosis inducer. Ferroptosis inducer-16 inhibits DNA synthesis and colony formation. Ferroptosis inducer-16 disrupts lysosomal integrity by releasing NO, triggers iron overload and oxidative stress, downregulates the SLC7A11-GPX4 axis, depletes GSH, and accumulates lipid peroxides. Ferroptosis inducer-16 inhibits tumor growth in an OVCAR8/ADR xenograft mouse model without obvious toxicity, and can be used in the study of non-small cell lung cancer and drug-resistant ovarian cancer.