2. Signaling Pathways
  3. Apoptosis
  4. 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 (117):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B1218R
    Sulfaphenazole (Standard)
    		Inhibitor
    Sulfaphenazole (Standard) is the analytical standard of Sulfaphenazole. This product is intended for research and analytical applications. 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 (Standard)
  • HY-100573A
    (E/Z)-Necrosulfonamide
    		Inhibitor 98.84%
    (E/Z)-Necrosulfonamide is a racemic compound of Necrosulfonamide (HY-100573). Necrosulfonamide, a necroptosis and gasdermin D inhibitor, selectively targets (MLKL). Necrosulfonamide prevents the MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a key substrate of RIP3 in the induction of necrosis.
    (E/Z)-Necrosulfonamide
  • HY-N10319
    Artepillin C
    		Inducer
    Artepillin C is an orally active CREB/CRTC2 inhibitor and TRPA1 covalent agonist (EC50=1.8 μM). Artepillin C inhibits CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression to regulate glucose and lipid metabolism. Artepillin C can also activate TRPA1 channels to induce spicy taste signals. Artepillin C can inhibit tumor cell proliferation, induce necroptosis, improve insulin resistance and inhibit liver lipid synthesis. Artepillin C can be used in the study of metabolic syndrome, tumor prevention and treatment, and inflammation.
    Artepillin C
  • HY-B0863S2
    Glyphosate-d2-1
    		Inducer 99.89%
    Glyphosate-d2-1 is the deuterium labeled Glyphosate. Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants.
    Glyphosate-d<sub>2</sub>-1
  • HY-100573S
    Necrosulfonamide-d4
    		Inhibitor 99.26%
    Necrosulfonamide-d4 is the deuterium labeled Necrosulfonamide (HY-100573). Necrosulfonamide, a necroptosis and gasdermin D inhibitor, selectively targets (MLKL). Necrosulfonamide prevents the MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a key substrate of RIP3 in the induction of necrosis.
    Necrosulfonamide-d<sub>4</sub>
  • HY-B1145S
    Chlorhexidine-d8 dihydrochloride
    		Inducer
    Chlorhexidine-d8 (dihydrochloride) is the deuterium labeled Chlorhexidine dihydrochloride (HY-B1145). Chlorhexidine dihydrochloride is a orally active cationic antimicrobial agent that targets microbial cell membranes. Chlorhexidine dihydrochloride binds to cell membrane phospholipids non-specifically, destroys membrane structure and induces leakage of cell contents. Chlorhexidine dihydrochloride has broad-spectrum bactericidal activity against both Gram-positive and Gram-negative bacteria. Chlorhexidine dihydrochloride can interfere with membrane permeability, cause protein precipitation and energy metabolism disorders, such as rapid inhibition of microbial growth and induction of cell death (necrosis or apoptosis).
    Chlorhexidine-d<sub>8</sub> dihydrochloride
  • HY-B0863S3
    Glyphosate-13C2,15N
    		Inducer ≥98.0%
    Glyphosate-13C2,15N is the 13C and 15N labled Glyphosate (HY-B0863). Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants.
    Glyphosate-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
  • 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-B0863S
    Glyphosate-d2
    		Inducer 99.73%
    Glyphosate-d2 is the deuterium labeled Glyphosate. Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants.
    Glyphosate-d<sub>2</sub>
  • HY-136509
    CIL62
    		Inducer
    CIL62 is a caspase-3/7-independent cell death inducer. The mechanism of action of CIL62 is Necrostatin-1 dependent cell death.
    CIL62
  • HY-W010201R
    Citronellol (Standard)
    		Inducer
    Citronellol (Standard) is the analytical standard of Citronellol. Citronellol (Standard) is an orally active inducer of apoptosis. Citronellol (Standard) can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol (Standard) can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol (Standard) can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol (Standard) exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.
    Citronellol (Standard)
  • 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-106777
    Cyclopentenylcytosine
    		Inducer 99.76%
    Cyclopentenylcytosine (CPC) is a nucleoside analog that reduces the levels of cytidine triphosphate (CTP) and deoxycytidine triphosphate (dCTP) in leukemic cells by inhibiting CTP synthetase. Cyclopentenylcytosine also promotes the phosphorylation of 1-β-D-arabinorubosylmannosylcytidine (araC) and its DNA intercalation activity. Cyclopentenylcytosine induces apoptosis and necrosis in the human T lymphocyte line MOLT-3 in a concentration (50-300 nM) and time (8-16 h) dependent manner. Co-treatment of cyclopentenylcytosine with araC enhances the effects of induction of apoptosis and necrosis, as well as its cytotoxicity in T lymphoblasts.
    Cyclopentenylcytosine
  • HY-W010800R
    Cholesteryl hemisuccinate (Standard)
    		Inhibitor
    Cholesteryl hemisuccinate (Standard) is the analytical standard of Cholesteryl hemisuccinate. This product is intended for research and analytical applications. 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[1][2].
    Cholesteryl hemisuccinate (Standard)
  • HY-B0339S
    Primidone-d5
    		Inhibitor ≥99.00%
    Primidone-d5 is the deuterium labeled Primidone. Primidone is the orally active inhibitor for TRPM3 (IC50 = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent.
    Primidone-d<sub>5</sub>
  • HY-148382
    RI-962
    		≥98.0%
    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-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-169509
    Topoisomerase I/II inhibitor 8
    		Inducer
    Topoisomerase I/II Inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of Topoisomerase I/II, capable of inducing DNA damage and PARP-1 activation, which subsequently leads to the activation of RIPK1, RIPK3, and MLKL, ultimately triggering necroptosis. Topoisomerase I/II Inhibitor 8 demonstrates remarkable anticancer activity by effectively targeting the nuclei of cancer cells and inducing cell death through necroptosis, showing great clinical potential in circumventing drug resistance in cancer treatment.
    Topoisomerase I/II inhibitor 8
  • 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
  • HY-149407
    Multi-kinase-IN-4
    		Activator
    Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, 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