1. Signaling Pathways
  2. Apoptosis
  3. Necroptosis

Necroptosis

Necroptosis is a form of regulated necrotic cell death mediated by receptor-interacting serine-threonine kinase 3 (RIPK3) and mixed lineage kinase domain-like (MLKL) and generally manifests with morphological features of necrosis. Necroptosis is characterized by early loss of plasma membrane integrity, leakage of intracellular contents, and organelle swelling. The cells dying through necroptosis lack the typical apoptotic characteristics, such as membrane blebbing, chromatin condensation, and intranucleosomal DNA cleavage into 180 bp DNA laddering, but may show TUNEL positivity.

Necroptosis triggers innate immune responses by rupturing dead cells and releasing intracellular components, it can be caused by Toll-like receptor (TLR)-3 and TLR-4 agonists, tumor necrosis factor (TNF), certain microbial infections, and T cell receptors. Necroptosis signaling is modulated by receptor-interacting protein kinase (RIPK) 1 when the activity of caspase-8 becomes compromised. Activated death receptors (DRs) cause the activation of receptor-interacting serine-threonine kinase 1 (RIPK1) and the RIPK1 kinase activity-dependent formation of an RIPK1-RIPK3-MLKL, which is complex II. RIPK3 phosphorylates MLKL, ultimately leading to necrosis through plasma membrane disruption and cell lysis.

Necroptosis Related Products (42):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-14909
    Bardoxolone
    Inhibitor 99.14%
    Bardoxolone (CDDO) is a novel nuclear regulatory factor (Nrf-2) activator for the study of chronic kidney disease. Bardoxolone is a potent necroptosis inhibitor that inhibits Z-VAD-FMK-induced necroptosis.
    Bardoxolone
  • HY-B1218
    Sulfaphenazole
    Inhibitor 99.83%
    Sulfaphenazole is a selective inhibitor of human cytochrome P450 (CYP) 2C9 enzyme. Sulfaphenazole is a cytoprotective agent against light-induced death of photoreceptors. Sulfaphenazole inhibits light-induced necrosis and mitochondrial stress-initiated apoptosis. Sulfaphenazole is an off patent sulfonamide antibiotic and demonstrates bactericidal activity through enhanced M1 macrophage activity. Sulfaphenazole can significantly reduce infarct size and restore post-ischemic coronary flow following ischemia and reperfusion.
    Sulfaphenazole
  • HY-144828
    RIP1/RIP3/MLKL activator 1
    Inducer
    RIP1/RIP3/MLKL activator 1 (Compound 6i) is a potent anti-glioma agent. RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway. RIP1/RIP3/MLKL activator 1 exerts acceptable BBB permeability.
    RIP1/RIP3/MLKL activator 1
  • HY-Y0698
    Thioacetamide
    ≥98.0%
    Thioacetamide (TAA) is an indirect hepatotoxin and causes parenchymal cell necrosis. Thioacetamide requires metabolic activation by microsomal CYP2E1 to thioacetamide-S-oxide initially and then to thioacetamide-S-dioxide, which is a highly reactive metabolite, and its reactive metabolites covalently bind to proteins and lipids thereby causing oxidative stress and centrilobular necrosis. Thioacetamide can induce chronic liver fibrosis, encephalopathy and other events model.
    Thioacetamide
  • HY-134050
    Apostatin-1
    Inhibitor 99.24%
    Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N (KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination of RIPK1 and beclin 1. Apostatin-1 blocks apoptosis and restores cellular homeostasis by activating autophagy in cells with accumulated mutant tau, α-synuclein, or huntingtin.
    Apostatin-1
  • HY-156087G
    Cholicamideβ (GMP)
    Inducer
    Cholicamideβ (GMP) is a GMP grade of Cholicamideβ. Cholicamideβ (compound 6) is a self-assembling, small molecule, cancer vaccine adjuvant. Cholicamideβ can form virus-like particles with low cytotoxicity. Cholicamideβ, upon binding to peptide antigens, enhances antigen presentation by dendritic cells and induces antigen-specific T cells. Cholicamideβ can induce apoptosis and necrosis.
    Cholicamideβ (GMP)
  • HY-149407
    Multi-kinase-IN-4
    Activator
    Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2/KDR/Flk-1, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer.
    Multi-kinase-IN-4
  • HY-162097
    RIPK1-IN-20
    Inhibitor
    RIPK1-IN-20 (compound 13c) has a favorable RIPK1 kinase inhibition activity with an IC50 value of 59.8 nM. RIPK1-IN-20 blocks TNFα-induced necroptosis in both human and murine cells (EC50=1.06–4.58 nM).
    RIPK1-IN-20
  • HY-W010800
    Cholesteryl hemisuccinate
    Inhibitor ≥98.0%
    Cholesteryl hemisuccinate is a with hepatoprotective an anticancer activity. Cholesteryl hemisuccinate inhibits Acetaminophen (AAP, HY-66005) hepatotoxicity, and prevents AAP-induced hepatic apoptosis and necrosis. Cholesteryl hemisuccinate inhibits DNA polymerase and DNA topoisomerase to inhibit DNA replication and repair and cell division. Thus, Cholesteryl hemisuccinate inhibits tumor growth.
    Cholesteryl hemisuccinate
  • HY-B0608
    Chlorhexidine (digluconate)
    Inducer ≥98.0%
    Chlorhexidine digluconate is a chlorophenyl biguanide with broad antibacterial action against both Gram (+) and (-) bacteria and fungi. Chlorhexidine digluconate is a broad-spectrum antiseptic and disinfectant. Chlorhexidine digluconate is effective to prevent and control infectious diseases of the mouth by killing bacteria in saliva and tongue. Chlorhexidine digluconate is a cytotoxic agent and induces cell necrosis and apoptosis.
    Chlorhexidine (digluconate)
  • HY-108351
    IM-54
    99.31%
    IM-54 is a selective inhibitor of oxidative stress-induced necrosis. IM-54 shows potent inhibitory activity against H2O2-induced necrosis. IM-54 acts as a potential cardioprotective agent and biological tool for investigating the molecular mechanisms of cell death.
    IM-54
  • HY-117200
    Necrostatin-7
    Inhibitor ≥98.0%
    Necrotatin-7 (Nec-7) is a potent necroptosis inhibitor with an EC50 of 10.6 μM. Necrotatin-7 does not inhibit recombinant RIP1 kinase.
    Necrostatin-7
  • HY-12456
    Duocarmycin SA
    Inducer ≥98.0%
    Duocarmycin SA is an orally active antitumor antibiotic with an IC50 of 10 pM. Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro.
    Duocarmycin SA
  • HY-124546
    Necrostatin-5
    Inhibitor 98.43%
    Necrostatin-5 (Nec-5) is a potent necroptosis inhibitor with an EC50 value of 0.24 µM. Necrostatin-5 also is a RIP1 inhibitor. Necrostatin-5 shows cardioprotective effects.
    Necrostatin-5
  • HY-135826
    Necroptosis-IN-1
    Inhibitor 98.39%
    Necroptosis-IN-1, an analog of Necrostatin-1, is a potent necroptosis inhibitor. Necroptosis-IN-1 is a RIPK inhibitor.
    Necroptosis-IN-1
  • HY-N3417
    Kongensin A
    Inhibitor ≥98.0%
    Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications.
    Kongensin A
  • HY-149258
    KWCN-41
    Inhibitor 99.83%
    KWCN-41 is a selective and efficient inhibitor of RIPK1 kinase with an IC50 value of 88 nM. KWCN-41 specifically inhibits cell necrosis but does not inhibit apoptosis. KWCN-41 also has anti-inflammatory effects.
    KWCN-41
  • HY-148454
    Necroptosis-IN-3
    Inhibitor 99.77%
    Necroptosis-IN-3 (Compound 69) is a necroptosis inhibitor that inhibits TNF-α induced necroptosis. Necroptosis-IN-3 (Compound STX1638) also inhibits 11β-HSD1.
    Necroptosis-IN-3
  • HY-148382
    RI-962
    RI-962 is a potent and selective receptor-interacting protein kinase 1 (RIPK1) inhibitor. RI-962 inhibits RIPK1 with an IC50 value of 35.0 nM. RI-962 can be used for the research of nervous system diseases and inflammatory diseases.
    RI-962
  • HY-153435
    RIP1 kinase inhibitor 5
    Inhibitor
    RIP1 kinase inhibitor 5 (example 1) is a potent inhibitor of RIP1, which is used as a checkpoint kinase to control tumor immunity. RIP1 kinase inhibitor 5 is similar with SIR1-365 (compound 13), which inhibits necrosis and iron death activity.
    RIP1 kinase inhibitor 5