Ferroptosis Inducer

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.

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.

Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 25.8 μM; is a widely used antipyretic and analgesic agent.. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor. Acetaminophen induces ferroptosis and leads to acute liver injury in mice model.

Ammonium iron(III) citrate (Ammonium ferric citrate), a physiological form of nonetransferrin-bound iron, induces intracellular iron overload to cause ferroptosis. Ammonium iron(III) citrate can enhance protein production.

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.

Itaconic acid, a precursor of polymers, chemicals, and fuels, can be synthesized by many fungi. Itaconic acid also is a macrophage-specific metabolite. Itaconic acid mediates crosstalk between macrophage metabolism and peritoneal tumors. Itaconic acid has anti-inflammatory, anti-microbial and immunomodulatory effect.

JKE-1674 is an orally active glutathione peroxidase 4 (GPX4) inhibitor and an active metabolite of GPX4 inhibitor ML-210. JKE-1674, an analog of ML-210 in which the nitroisoxazole ring is replaced with an α-nitroketoxime. JKE-1674 can convert into a nitrile oxide JKE-1777. JKE-1674 kills LOX-IMVI cells in a manner that is equipotent to ML-210 and is completely rescued by ferroptosis inhibitors.

Erastin2, an Erastin (HY-15763) analog, is a ferroptosis inducer and a potent, selective inhibitor of the system xc(-) cystine/glutamate transporter

Ogremorphin (OGM) is a G protein coupled sensor GPR68 inhibitor with anti-inflammatory and anti-tumor activities. Ogremorphin can inhibit the migration of human melanoma cells and induce ferroptosis in glioblastoma cells.

FSEN1 is a potent and non-competitive FSP1 inhibitor with an IC₅₀ value of 313 nM. FSEN1 triggers iron death in cancer cells by inhibiting FSP1. FSEN1 can be used in research of cancer.

GPX4-IN-3 (26a) is a potent glutathione peroxidase 4 (GPX4) inhibitor as a selective ferroptosis inducer. GPX4-IN-3 (26a) exhibits 71.7% inhibition for GPX4 with 1 μM.

N6F11 is a selective ferroptosis inducer, and can selectively induce ferroptosis by targeting TRIM25-mediated GPX4 degradation in cancer cells while sparing immune cells. N6F11 initiates HMGB1-dependent antitumor immunity mediated by CD8⁺ T cells.

Solasonine is a ferroptosis inducer which can be isolated from Solanum melongena that has anti-infection, anti-cancer, and neurogenesis promoting properties. Solasonine promotes ferroptosis of HCC cells via destruction of the glutathione redox system induced by inhibiting GPX4, and can be used for cancer research.

Ferumoxytol is an FDA-approved ultrasmall superparamagnetic iron oxide preparation and iron replacement agent that exerts selective activity against leukemia cells with low ferroportin expression. Ferumoxytol increases intracellular iron levels, induces reactive oxygen species (ROS) production via the Fenton reaction, and triggers oxidative stress and cell death. Ferumoxytol reduces disease burden in mouse models and patient-derived leukemia models. As an MRI contrast agent, Ferumoxytol enables imaging of vascular lesions, tumors and lymph nodes. Ferumoxytol can be used in research related to acute myeloid leukemia and blast-phase chronic myeloid leukemia.

TASIN-30 is a selective EBP inhibitor with an EC₅₀ of 0.097 μM. TASIN-30 blocks the production of 7-dehydrocholesterol (7-DHC) and downstream cholesterol biosynthesis processes. TASIN-30 depletes downstream sterols, disrupts the integrity of lipid rafts in tumor cells, accelerates intracellular cholesterol consumption, and inhibits tumor cell proliferation. TASIN-30 induces ferroptosis and apoptosis by reducing 7-DHC levels and increasing phospholipid peroxidation. TASIN-30 achieves tumor suppression in nude mice with osteosarcoma. TASIN-30 can be used in cancer-related research such as colorectal cancer and osteosarcoma.

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.

Itaconic acid (Standard) is the analytical standard of Itaconic acid. This product is intended for research and analytical applications. Itaconic acid, a precursor of polymers, chemicals, and fuels, can be synthesized by many fungi. Itaconic acid also is a macrophage-specific metabolite. Itaconic acid mediates crosstalk between macrophage metabolism and peritoneal tumors. Itaconic acid has anti-inflammatory, anti-microbial and immunomodulatory effect.

Formosanin C is a diosgenin saponin with multiple biological activities. Formosanin C possesses multiple anti-tumor mechanisms, including inducing apoptosis and autophagy, blocking the cell cycle, inhibiting metastasis and inducing ferroptosis. Formosanin C can inhibit the NF-κB signaling pathway to exert anti-inflammatory effects, and enhance the activity of immune cells. Formosanin C exhibits the inhibiting effect against C. albicans. Formosanin C can be used for the study of anti-inflammation, antifungal anti and anti-cancer (including lung cancer, liver cancer, breast cancer and colorectal cancer, etc.).

GPX4-IN-5 is a covalent inhibitor of GPX4 (IC₅₀: 0.12 μM). GPX4-IN-5 can induce ferroptosis and has anti-tumor effects. GPX4-IN-5 can be used in the study of triple-negative breast cancer (TNBC).

KY386 is a DHX33 helicase inhibitor with an IC₅₀ of 0.019 μM. KY386 inhibits the cell viability of various cancer cells. KY386 induces ferroptosis in cancer cells, and induces apoptosis in some cancer cell lines. KY386 increases the intracellular levels of ROS, LPO and Fe²⁺, and decreases the level of GSH in cancer cells. KY386 inhibits the growth of gastric cancer and colon cancer xenografts in nude mice. KY386 is applicable to the related research on liver cancer, lung cancer, pancreatic cancer, colorectal cancer, gastric cancer, breast cancer, leukemia, renal cancer, prostate cancer, esophageal cancer, cervical cancer, brain cancer (glioblastoma) and melanoma.