Ferroptosis Inducer

GPX4-IN-19 is an effective GPX4 inhibitor (IC₅₀ = 0.311 μM), covalently binds to the Sec 46 site of GPX4. GPX4-IN-19 shows strong anti-proliferative activity with high ferroptosis selectivity. GPX4-IN-19 causes intracellular Fe²⁺ accumulation, leading to increased levels of lipid peroxides (LPOs) and reactive oxygen species (ROS), which induces ferroptosis and subsequently results in DNA damage. GPX4-IN-19 can be used for the study of Triple-Negative Breast Cancer (TNBC).

Ferroptosis inducer-1 (compound BX-3a) is a Ferroptosis inducer with antitumor potential. Ferroptosis inducer-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

NPD4928, a GPX4 inhibitor, enhances RSL3 (HY-100218A)-dependent ferroptosis. NPD4928 binds to ferroptosis suppressor protein 1 (FSP1) and inhibits its enzymatic activity.

JST‑TfR09 (PPMX‑T003) is a human monoclonal antibody (mAb) targeting transferrin receptor 1 (TfR1/CD71). JST‑TfR09 blocks the binding of transferrin to TfR1, inhibits TfR1 internalization, and suppresses cellular iron uptake. JST‑TfR09 triggers ferritin degradation via activating the autolysosomal system, promotes ROS production and lipid peroxidation, and ultimately induces ferroptosis. JST‑TfR09 exhibits cytotoxicity toward human erythroblasts differentiated from hematopoietic stem cells. JST-TfR09 can be used in leukemia research. Recommended isotype control: Human IgG1 lambda, Isotype Control (HY-P99992).

Auriculasin is an anticancer agent that inhibits VEGFR2, PI3K/AKT/mTOR, MAPK. Auriculasin can inhibit cell proliferation, induce cell apoptosis, and inhibit angiogenesis, and promotes mitochondrial oxidative stress and ferroptosis. Auriculasin is also active at the cannabinoid receptor CB1 with an IC₅₀ of 8.92 μM. Auriculasin can be used in cancer research, especially related diseases such as prostate cancer and non-small cell lung cancer, as well as research on the development of anti-angiogenic drugs.

GPX4-IN-6 (Compound C25) is a GPX4 covalent inhibitor with an IC₅₀ value of 0.13 μM. GPX4-IN-6 (Compound C25) can induce ferroptosis for the research of triple-negative breast cancer (TNBC) .

Theasaponin E1 is an orally effective tea saponin. Theasaponin E1 inhibits the proliferation of cancer cells by activating apoptosis. Theasaponin E1 inhibits angiogenesis in ovarian cancer cells and HUVECs by reducing the expression of VEGF. Theasaponin E1 upregulates the phosphorylation level of ATM protein and the expression level of PTEN protein in cancer cells, decreases the phosphorylation levels of Akt, mTOR, p70S6K and 4E-BP1 proteins, downregulates the expression of HIF-1α and NF-κB, and reduces the protein expression of Notch ligands Dll4 and Jagged1. Theasaponin E1 exerts neuroprotective effects by inhibiting the activity of acetylcholinesterase, activating α-secretase and neprilysin, reducing the concentration of Aβ, and inhibiting the activities of β-secretase and γ-secretase. Theasaponin E1 exhibits toxic effects on cancer cells and quinone reductase-inducing activity, and inhibits tumor growth in vivo. Theasaponin E1 induces ferroptosis in Pomacea canaliculata by synergistically disrupting cholesterol homeostasis and sphingolipid metabolism. Theasaponin E1 possesses anti-biofilm activity against Candida albicans. Theasaponin E1 can be used in the research of ovarian cancer, obesity, Alzheimer's disease and fungal infections.

HDAC11-IN-3 (Compound A9) is a selective HDAC11 inhibitor (IC₅₀: 4.1 nM). HDAC11-IN-3 has inhibitory effects on U937 and OCI-AML2 acute myeloid leukemia (AML) cell lines (IC₅₀: 10 μM). HDAC11-IN-3 has significant anti-AML activity, inducing apoptosis, cell cycle arrest, and differentiation. HDAC11-IN-3 upregulates the iron transporters transferrin (TF) and transferrin receptor (TFRC), and activates the p62-Keap1-Nrf2-HMOX1 pathway, which together lead to increased intracellular iron levels and induce ferroptosis in AML cells. HDAC11-IN-3 can be used alone or in combination with Cytarabine (HY-13605) for AML research.

GPX4-IN-9 (Compound A16) is a glutathione peroxidase 4 (GPX4) inhibitor that specifically targets GPX4 under both in vitro and in vivo conditions, inducing ferroptosis. GPX4-IN-9 exhibits cytotoxicity against pancreatic cancer cells and can be used in cancer research.

Mg(Ⅱ)-EDTA (Ethylenediaminetetraacetic acid magnesium) disodium tetrahydrate is a divalent metal chelator and ferroptosis inducer. Mg (Ⅱ)-EDTA disodium tetrahydrate reduces E-cadherin expression by chelating Ca²⁺ on the surface of tumor cells, thereby triggering cell dissociation and inducing epithelial-mesenchymal transition (EMT). Mg (Ⅱ)-EDTA disodium tetrahydrate further chelates lysosomal iron to form EDTA-Fe, induces ferroptosis through the Fenton reaction, and synergistically enhances immune responses to inhibit tumor metastasis. Mg (Ⅱ)-EDTA (disodium tetrahydrate) can be used in tumor-related research.

W1131 TFA is a potent STAT3 inhibitor that induces ferroptosis. W1131 inhibits cancer progression in subcutaneous xenograft, organoid, and PDX models of gastric cancer. W1131 effectively alleviates cancer cell chemoresistance to 5-FU (HY-90006). W1131 regulates the cell cycle, DNA damage response, and oxidative phosphorylation, including the IL6-JAK-STAT3 pathway and the ferroptosis pathway.

Tralopyril is an orally active, blood-brain barrier-penetrating antifouling insecticide and endocrine disruptor. By interfering with the thyroid hormone system and mitochondrial oxidative phosphorylation, Tralopyril downregulates the transcription of genes such as TRHR, Nkx2.1, TRα and induces ferroptosis. Tralopyril disrupts amino acid, energy and lipid metabolism, exhibits significant skeletal and reproductive toxicity, and causes developmental damage. Tralopyril has a long half-life in vivo and wide tissue distribution, posing potential risks to aquatic organisms and human health. Tralopyril shows species specificity in in vitro liver microsomal metabolism, exerts lethal effects on target insects and laboratory animals, and is commonly used in studies of chlorfenapyr poisoning and related toxic mechanisms.

1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-Pe is a phospholipid that contains stearic acid (HY-B2219) at the sn-1 position and 15(S)-HpETE at the sn-2 position. It is produced via oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-Pe (SAPE) by 15-lipoxygenase (15-LO). 1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-Pe (0.6 and 0.9 μM) increases ferroptotic cell death in wild-type and Acsl4 knockout Pfa1 mouse embryonic fibroblasts (MEFs) treated with the GPX4 inhibitor RSL3.

HDAC11-IN-5 is a selective, potent and orally active HDAC11 inhibitor with an IC₅₀ of 0.021 μM. HDAC11-IN-5 increases fatty acylation levels of substrate SHMT2 in AML cells. HDAC11-IN-5 induces apoptosis, G1 phase cell cycle arrest, ferroptosis, ROS production and terminal myeloid differentiation in AML cells. HDAC11-IN-5 demonstrates anti-tumor potency in an MLL-AF9-induced mouse AML model. HDAC11-IN-5 can be used for the research of cancer, such as acute myeloid leukemia.

PROTAC GPX4 degrader-4 is a potent GPX4 PROTAC degrader, with DC₅₀ values of 1366.67 nM and 475.15 nM in T24 and RT4 cells, respectively. PROTAC GPX4 degrader-4 targets and degrades GPX4 protein via the ubiquitin-proteasome system, thereby inducing cellular ferroptosis. PROTAC GPX4 degrader-4 can be used for research on bladder cancer.

BCP-T.A, a tunable heterocyclic electrophile, is a potent ferroptosis inducer by binding to GPX4. BCP-T.A is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Tubulin inhibitor 30 (Compound 15) is a tubulin assembly inhibitor with an IC₅₀ of 0.52 μM. Tubulin inhibitor 30 can induce ferroptosis.

RSL3-NH2 hydrochloride is a GPX4 inhibitor and ferroptosis inducer. RSL3-NH2 hydrochloride triggers the iron-dependent cell death pathway associated with lipid peroxidation by inhibiting GPX4 activity. RSL3-NH2 hydrochloride exhibits significant cytotoxicity against colorectal cancer cells and effectively induces their ferroptosis. RSL3-NH2 hydrochloride can serve as a ADC payload for synthesizing a ADC and be used in colorectal cancer-related research.

Diplacone is an orally active geranyl flavanone. It is isolated from the fruits of Paulownia tomentosa. Diplacone reduces COX-2 levels and increases the pro-MMP2/MMP2 ratio. It induces ferroptosis-mediated cell death. Diplacone enhances mitochondrial Ca²⁺ influx and ROS production. It possesses anti-inflammatory and free radical-scavenging activities. Diplacone can be used in research related to ulcerative colitis and non-small cell lung cancer.

Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer.