Ferroptosis Inducer

KY0418 is a selective GPX4 inhibitor. KY0418 selectively and covalently modifies the selenocysteine residue of GPX4 and inhibits GPX4 activity. KY0418 induces ferroptosis and suppresses cell proliferation. KY0418 can be used for the study of ferroptosis and cancer.

Anticancer agent 239 (Compound 5) is a ligand of hTERT promoter G-quadruplex DNA structures (hTERT G4) (K_d = 1.1 μM), and downregulates hTERT expression. Anticancer agent 239 decreases telomerase activity, shortens telomere length, and induces DNA damage, acute cellular senescence, and apoptosis. Anticancer agent 239 causes mitochondrial dysfunction, disrupts iron metabolism and activates ferroptosis in cancer cells. Anticancer agent 239 inhibits tumor growth in MDA-MB-231 xenograft mouse model.

Antitumor agent-217 is a dual mitochondria-targeted anticancer agent. Antitumor agent-217 exhibits potent and selective antiproliferative activity against bladder cancer cell line J82 (IC₅₀ = 6.3 μM), and inhibits colony formation and migration of J82 cells. Antitumor agent-217 accumulates in mitochondria, alters mitochondrial morphology, reduces ATP production, increases ROS generation and decreases mitochondrial membrane potential. Antitumor agent-217 induces apoptosis (Apoptosis) and ferroptosis (Ferroptosis) in bladder cancer cells. Antitumor agent-217 can be used for the research of bladder cancer.

CAR-2 is a BODIPY-based photosensitizer that induces ferroptosis in photodynamic therapy (PDT) by targeting the endoplasmic reticulum (ER) and lipid droplets (LDs). CAR-2 exhibits phototoxicity in breast cancer cells with IC₅₀ of 0.01-0.02 μM. CAR-2 exhibits antitumor efficacy in 4T1 xenograft mouse models.

PROTAC FSP1 degrader 1 is a highly efficient and selective PROTAC degrader targeting FSP1. PROTAC FSP1 degrader 1 significantly induces the accumulation of intracellular lipid peroxides. PROTAC FSP1 degrader 1 exhibits synergistic induction of ferroptosis with GPX4 inhibitors. PROTAC FSP1 degrader 1 can induce ROS production. PROTAC FSP1 degrader 1 upregulates the mRNA expression of ferroptosis-related proteins (GPX4, FTH1, ACSL4, TfR1, FSP1). PROTAC FSP1 degrader 1 can be used for the study of triple-negative breast cancer.

ZX782 is a HyT GPX4 degrader and a ferroptosis inducer, which induces GPX4 degradation and significantly increases lipid ROS accumulation in HT1080 cells. ZX782 can be used to treat AD by reducing the size and/or number of brain amyloid plaques and by inhibiting the spread of IL-1beta-positive microglial-like cells around amyloid plaques. ZX782 is labeled with hydrophobic benzyl alcohol (HBA) and appears bright blue under acidic conditions, which can be used for quantitative determination. ZX782 is composed of target protein ligand (red part) ML-210 (HY-100003), PROTAC linker (black part) Bromo-PEG2-CH2-Boc (HY-141371) and Hty molecule (blue part) Adamantan-1-ylmethanamine (HY-W037848). The conjugate consisting of Hyt and linker parts is Adamantan-C-amide-PEG2-C-Br (HY-161974), and the activity control of the target protein ligand is Hydroxyl-ML-210 (HY-161973).

Piperazine Erastin (Standard) is the analytical standard of Piperazine Erastin (HY-100887). This product is intended for research and analytical applications. Piperazine erastin is an analog of erastin which induces an iron-dependent form of non-apoptotic cell death, termed ferroptosis. Piperazine erastin can be used in cancer research.

Cephaeline ((-)-Cephaeline), a desmethyl analog of Emetine, is a phenolic alkaloid in Indian Ipecac roots isolated from the Cephaelis ipecacuanha. Cephaeline exhibits potent inhibition of both Zika virus (ZIKV) and Ebola virus (EBOV) infections. Cephaeline is an inductor of histone H3 acetylation and an inhibitor of mucoepidermoid carcinoma cancer stem cells (MEC), which promotes ferroptosis by inhibiting NRF2 to exert anti-lung cancer efficacy.

Ferrous gluconate (Standard) is the analytical standard of Ferrous gluconate. This product is intended for research and analytical applications. Ferrous gluconate is a highly water-soluble iron-containing agent with high bioavailability and bactericidal activity. As a non-heme iron, Ferrous gluconate is used for meat product fortification and improvement of iron deficiency anemia. Ferrous gluconate induces ferroptosis in E. coli through Fe²⁺ infiltration, reactive oxygen species burst, lipid peroxidation and direct interaction with DNA. Ferrous gluconate also downregulates the SOS responsive transcriptional repressor LexA. In addition, Ferrous gluconate regulates multiple key pathways in E. coli such as fatty acid metabolism, iron-sulfur cluster assembly and pyruvate metabolism, and is applied in studies related to *E. coli* infection and iron deficiency anemia.

GPX4-IN-13 (compound 16) is a GPX4 inhibitor with anticancer activity. GPX4-IN-13 reduces thyroid cell proliferation and induces ferroptosis by inhibiting the expression level of GPX4. GPX4-IN-13 inhibits the growth of three thyroid cancer cell lines: N-thy-ori-3-1 (IC₅₀=8.39 μM), MDA-T32 (IC₅₀=10.28 μM) and MDA-T41 (IC₅₀=8.18 μM).

Diphenyl disulfide (Standard) is an analytical standard for diphenyl disulfide (HY-Y1177). This product is intended for research and analytical applications. Diphenyl disulfide (Phenyl disulfide) is an organic disulfide compound. Diphenyl disulfide inhibits the PI3K/AKT/mTOR pathway, and induces ferroptosis (ferroptosis), apoptosis (apoptosis) and autophagy (autophagy) in cancer cells. Diphenyl disulfide downregulates GPX4 expression, inhibits NRF2 phosphorylation, induces lipid peroxidation, promotes xCT ubiquitination, induces proteolytic cleavage of p21 Bax into p18 Bax, and suppresses cell proliferation and viability. Diphenyl disulfide can be used in research related to melanoma and breast cancer.

Imidazole ketone erastin (Standard) is the analytical standard of Imidazole ketone erastin (HY-114481). This product is intended for research and analytical applications. Imidazole ketone erastin is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system x_c^- and an activator of ferroptosis. Imidazole ketone erastin has anti-tumor activity.

Chloranil (Standard) is the analytical standard of Chloranil. This product is intended for research and analytical applications. Chloranil, an orally active metabolite of pentachlorophenol and hexachlorobenzene, is a widely used fungicide. Chloranil can induce ROS production. Chloranil induces neutrophil extracellular traps through the ROS-JNK-NOX2 pathway. Chloranil induces ferroptosis and neuroinflammation. Chloranil induces apoptosis of mouse embryonic stem cells.

2-Hydroxyanthraquinone (Standard) is the analytical standard of 2-Hydroxyanthraquinone (HY-W012352). This product is intended for research and analytical applications. 2-Hydroxyanthraquinone is a product generated by the photochemical oxidation of Anthracene (ANT) (HY-Y0299). 2-Hydroxyanthraquinone induces ferroptosis in cardiomyocytes by depleting GSH and inhibiting GPX4, leading to cardiac developmental malformations. 2-Hydroxyanthraquinone causes damage to the cerebrovascular system and blood-brain barrier in zebrafish by downregulating the Wnt/β-catenin signaling pathway, as well as inducing inflammation and neuronal apoptosis. 2-Hydroxyanthraquinone can be used in studies related to cerebrovascular diseases and cardiotoxicity.

Curcumenol (Standard) ((+)-Curcumenol (Standard)) is the analytical standard of Curcumenol (HY-N2259). This product is intended for research and analytical applications. Curcumenol ((+)-Curcumenol) is a natural compound with oral efficacy, exhibiting an IC₅₀ of 12.6 μM and a K_i of 10.8 μM against human CYP3A4. Curcumenol inhibits TNFα-induced phosphorylation/degradation of IκBα, phosphorylation/nuclear translocation of NF-κB p65, as well as the upregulation of MMP3, MMP9, MMP13, TRAF3, IL1RL1, TNFα and IL-1β. Curcumenol suppresses LPS-induced phosphorylation of Akt and p38 MAPK, as well as the production of pro-inflammatory mediators/proteins, and downregulates the SLC7A11/NF-κB/TGF-β pathway. Curcumenol binds to and inhibits the activation of Fyn and Lyn, blocks the function of downstream FcεRI signaling components, and reduces the release of allergic mediators/cytokines. Curcumenol upregulates the expression of KDM6B, and promotes chondrocyte proliferation and cartilage repair. Curcumenol induces ferroptosis and apoptosis, regulates the EMT process, and inhibits tumor growth and metastasis of triple-negative breast cancer. Curcumenol possesses anti-inflammatory, neuroprotective, antioxidant, antitumor, antiviral and hepatoprotective activities. Curcumenol can be used in research related to intervertebral disc degeneration, cancer, inflammation, central nervous system neurodegenerative diseases, allergic reactions and knee osteoarthritis.