2. Signaling Pathways
  3. Apoptosis
  4. Ferroptosis

Ferroptosis

Ferroptosis

Ferroptosis

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Ferroptosis is a non-apoptotic form of regulated cell death. It is distinct from other regulated cell death phenotypes, such as apoptosis and necroptosis. Ferroptosis is characterized by extensive lipid peroxidation, which can be suppressed by iron chelators or lipophilic antioxidants. Mechanistically, Ferroptosis inducers are divided into two classes: (1) inhibitors of cystine import via system xc− (e.g., Erastin), which subsequently causes depletion of glutathione (GSH), and (2) covalent inhibitors (e.g., (1S, 3R)-RSL3) of glutathione peroxidase 4 (GPX4). Since GPX4 reduces lipid hydroperoxides using GSH as a co-substrate, both compound classes ultimately result in loss of GPX4 activity, followed by elevated levels of lipid reactive oxygen species (ROS) and consequent cell death.

Ferroptosis is an iron- and ROS-dependent form of regulated cell death (RCD). Misregulated Ferroptosis has been implicated in multiple physiological and pathological processes, including cancer cell death, neurotoxicity, neurodegenerative diseases, acute renal failure, drug-induced hepatotoxicity, hepatic and heart ischemia/reperfusion injury, and T-cell immunity.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-100329
    CGP 65015
    		Inhibitor
    CGP 65015 is an oral iron chelator, which can mobilize iron deposits.
    CGP 65015
  • HY-W509563
    Frataxin-IN-1
    Frataxin-in-1 (Compound (+)-11) is a Frataxin inhibitor with IC50 value of 45 μM, which can be used in the study of Friedreich's ataxia (FRDA).
    Frataxin-IN-1
  • HY-162867
    Photosensitizer-5
    		Inducer
    Photosensitizer-5 is a photosensitizer. Photosensitizer-5 has cytotoxicity against HeLa and HepG2 cells, with IC50 values of 10.4 nM and 6.9 nM, respectively. Photosensitizer-5 can lead to lipid peroxidation and induces cell death through an iron-independent ferroptosis-like pathway. Photosensitizer-5 shows anti-tumor activity in HeLa tumor-bearing mice.
    Photosensitizer-5
  • HY-175826
    USP30-IN-20
    		Inducer
    USP30-IN-20 is an orally active USP30 inhibitor (Kd = 1.61 μM, IC50 = 12.8 μM). USP30-IN-20 induces ferroptosis by promoting ubiquitination-mediated degradation of GPX4. USP30-IN-20 inhibits the proliferation, migration, invasion, and stemness of prostate cancer cells. USP30-IN-20 induces G0/G1 cell cycle arrest and ROS levels in prostate cancer cells. USP30-IN-20 exhibits significant anti-tumor efficacy in PC3 cell subcutaneous xenografts in mice. USP30-IN-20 can be used for the study of advanced prostate cancer.
    USP30-IN-20
  • HY-155203
    Anticancer agent 154
    		Inducer
    Anticancer agent 154 (Compound 8h) increases the levels of reactive oxygen species and leads to mitochondrial damage. Anticancer agent 154 induces cell apoptosis and DNA damage. Anticancer agent 154 also induces ferroptosis by reducing the GSH level and GPX4 expression and increasing the lipid peroxidation level. Anticancer agent 154 inhibits cancer cell (HT29, H1975, A549, and MCF-7) proliferation with IC50s of 1.0-1.9 μM.
    Anticancer agent 154
  • HY-180245
    STAT3-IN-51
    		Inducer
    STAT3-IN-51 is a STAT3 inhibitor that directly binds to the STAT3 SH2 domain. STAT3-IN-51 induces apoptosis, ferroptosis, and immunogenic cell death (ICD) to potentiate anti-tumor immunity. STAT3-IN-51 inhibits STAT3 activation (phosphorylation, p-STAT3) and its downstream signaling. STAT3-IN-51 induces ROS generation, decreases Bcl-2 expression, disruptes mitochondrial function, suppresses GPX4 activity, and promotes lipid peroxidation. STAT3-IN-51 can be used for the study of colorectal carcinoma, breast adenocarcinoma, non-small cell lung cancer (NSCLC) and Cisplatin (HY-17394)-resistant pulmonary adenocarcinoma.
    STAT3-IN-51
  • HY-W342441
    Monosialoganglioside GM3 (bovine)
    		Inhibitor
    Monosialoganglioside GM3 (bovine) is a monosialoganglioside and an inhibitor of VEGFR2 and Akt. At a concentration of 20 μM, Monosialoganglioside GM3 inhibits angiogenesis and reduces the proliferation and migration of human umbilical vein endothelial cells (HUVECs) by inhibiting VEGFR2 and Akt phosphorylation. Ganglioside GM3 also inhibits ferroptosis, providing protective effects during the formation of abdominal aortic aneurysms. Additionally, Monosialoganglioside GM3 (bovine) acts as an inhibitor of insulin signaling, inducing the dissociation of the insulin receptor (IR)-Caveolin-1 complex from lipid microdomains and causing insulin resistance in adipocytes. Monosialoganglioside GM3 (bovine) can be used in cancer and metabolic disease research.
    Monosialoganglioside GM3 (bovine)
  • HY-163718
    Ferroptosis-IN-9
    		Inhibitor
    Ferroptosis-IN-9 (compound 23b) is a ferroptosis inhibitor with an IC50 value of >30uM for hERG inhibition. Ferroptosis-IN-9 is a ROS scavenger. Ferroptosis-IN-9 can be used in neurodegenerative disease research.
    Ferroptosis-IN-9
  • HY-183289
    Ferroptosis-IN-25
    		Inhibitor
    Ferroptosis-IN-25, Trolox (HY-101445) derivative, is a selective ferroptosis inhibitor. Ferroptosis-IN-25 selectively inhibits ferroptosis by scavenging ROS and suppressing lipid peroxidation independently of glutathion. Ferroptosis-IN-25 reduces corneal neovascularization and edema in murine corneal alkali burn models via topical administration.Ferroptosis-IN-25 can be used for the research of ocular surface diseases.
    Ferroptosis-IN-25
  • HY-N0683S1
    2-ambo-Vitamin E-13C3
    		Inhibitor
    α-Vitamin E-13C3 is the 13C-labeled α-Vitamin E. α-Vitamin E ((+)-α-Tocopherol), a naturally occurring vitamin E form, is a potent antioxidant.
    2-ambo-Vitamin E-<sup>13</sup>C<sub>3</sub>
  • HY-177483
    OART
    		Inducer
    OART (Oxaliplatin-artesunate) is a ferroptosis inducer. OART significantly inhibits tumor cell proliferation. OART induces cytoplasmic and mitochondrial LPO to promote tumor ferroptosis, via destroying glutathione-mediated ferroptosis defense system and enhancing iron-dependent Fenton reaction. OART enhances tumor immunogenicity, transforming tumor environment from immunosuppressive to immunosensitive. OART has strong tumor regression in tumor-bearing mouse models. OART can be used for cancer immunotherapy research.
    OART
  • HY-168030
    hCAIX-IN-23
    hCAIX-IN-23 (Compound 27) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 10.4 and 8.5 nM for hCA IX and hCA XII, respectively. In addition to inhibiting hCA activity, hCAIX-IN-23 releases NO, exhibiting dual antitumor activity. hCAIX-IN-23 induces apoptosis by regulating mitochondrial caspase activity and the ferroptosis pathway (ferroptosis) through the downregulation of hCA IX and iron-regulatory protein expression. hCAIX-IN-23 is useful for renal cancer research.
    hCAIX-IN-23
  • HY-173613
    VEGFR-2-IN-68
    		Inducer
    VEGFR-2-IN-68 (13b) is a VEGFR-2 inhibitor, with an IC50 of 41.51 nM. VEGFR-2-IN-68 (13b) induces apoptosis and G2/M phase arrest. VEGFR-2-IN-68 (13b) exhibits anti-metastatic properties in cancer cells.
    VEGFR-2-IN-68
  • HY-178370
    Ferroptosis inducer-12
    		Inducer
    Ferroptosis inducer-12 is a potent and selective ferroptosis inducer. Ferroptosis inducer-12 exhibits potent antiproliferative activity against HT1080 and OS-RC-2, with IC50 values of 3 nM and 5 nM, respectively. Ferroptosis inducer-12 strongly inhibits GPX4 enzymatic activity, induces intracellular ROS and elevates intracellular Fe2+ levels in OS-RC-2 cells. Ferroptosis inducer-12 significantly inhibits tumor growth in BALB/c nude mice bearing OS-RC-2 xenografts. Ferroptosis inducer-12 can be used for the study of cancer.
    Ferroptosis inducer-12
  • HY-168874
    TrxR1-IN-2
    		Inducer
    TrxR1-IN-2 (Compound 6a) is a TrxR1 inhibitor that covalently binds to the Cys475 and Sec498 sites of TrxR1, thereby inhibiting TrxR1 activity and leading to redox homeostasis disruption, which triggers apoptosis and ferroptosis.
    TrxR1-IN-2
  • HY-P10133
    PRDX3(103-112) SO3 modified, human
    PRDX3(103-112) SO3 modified, human is a marker of ferroptosis, and can be used for liver diseases study.
    PRDX3(103-112) SO3 modified, human
  • HY-178475
    CA IX/GPX4-IN-1
    		Inducer
    CA IX/GPX4-IN-1 (Compound 22abcb) is a dual targeted inhibitor of CA IX and GPX4 activity. CA IX/GPX4-IN-1 can effectively kill SUM159PT cells (IC50 = 416 nM) by inducing iron death under hypoxic conditions. CA IX/GPX4-IN-1 has an IC50 of 663 nM to CA IX in SUM159PT-CAIX-FL cells. CA IX/GPX4-IN-1 can significantly inhibit tumor growth and can be reversed by ferroptosis inhibitors. CA IX/GPX4-IN-1 can be used for research on breast cancer and other cancers.
    CA IX/GPX4-IN-1
  • HY-176220
    GPX4-AUTAC
    		Inducer
    GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader (AUTAC). GPX4-AUTAC consists of an inhibitor ML162-yne (HY-153748), a degradation tag FBnG (HY-W073762) and a glycol linker (HY-W021401). GPX4-AUTAC promotes the ubiquitination of GPX4 by E3 ligase TRAF6, and enhances the binding with GPX4 and p62, leading to the selective autophagy-dependent degradation of GPX4. GPX4-AUTAC significantly induces ferroptosis and shows a potent anti-cancer activity in breast cancer cells, breast cancer-derived organoids (PDOs) and MDA-MB-231 tumor xenograft mice model, with potent synergistic effects when combined with Sulfasalazine (SAS) (HY-14655) or chemotherapy drugs (Paclitaxel (HY-B0015) or Cisplatin (HY-17394)).
    GPX4-AUTAC
  • HY-155158
    Anticancer agent 147
    		Inducer
    Anticancer agent 147 (compound 6j) is a derivative of sophoridine (HY-N1373) and is a ferroptosis inducer. Anticancer agent 147 can promote the accumulation of intracellular Fe2+, reactive oxygen species (ROS) and MDA, increase ER stress, and upregulate the expression of the activating transcription factor ATF3. Anticancer agent 147 has good anti-liver cancer effects in vitro and in vivo.
    Anticancer agent 147
  • HY-178115
    MB-Buf
    		Inducer
    MB-Buf is a conjugation of methylene blue (HY-14536) and bufalin (HY-N0877) . MB-Buf can targeting degrade GPX4 upon light activation. MB-Buf can induce cell apoptosis, ferroptosis, and ROS production. MB-Buf can be used for the research of cancer, such as breast cancer.
    MB-Buf
Cat. No. Product Name / Synonyms Application Reactivity
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