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 (165):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-116107
    AG311
    		Inducer
    AG311 is an anticancer and antimetastatic agent. AG311 induces rapid necrosis in numerous cancer cell lines.
    AG311
  • HY-156920
    VDX-111
    		Inducer
    VDX-111 is an analog of vitamin D. VDX-111 exhibits cytotoxicity in ovarian cancer cells through upregulation of RIPK1/RIPK3 pathway and induction of necroptosis. VDX-111 promotes expressions of cytokines and exhibits antitumor activity in mouse model.
    VDX-111
  • HY-183797
    Antitumor agent-218
    		Inducer
    Antitumor agent-218 is an aggregation-induced emission (AIE)-based photosensitizer. Antitumor agent-218 selectively accumulates in the endoplasmic reticulum, and generates ROS within the endoplasmic reticulum upon irradiation to induce necroptosis of tumor cells. Antitumor agent-218 can be used in cancer-related research.
    Antitumor agent-218
  • HY-155804
    RIP1 kinase inhibitor 8
    		Inhibitor
    RIP1 kinase inhibitor 8 (Compound 77) is a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor with an IC50 of 20 nM. RIP1 kinase inhibitor 8 prevents necrotic cell death. RIP1 kinase inhibitor 8 shows a favorable pharmacokinetic profile in multiple species.
    RIP1 kinase inhibitor 8
  • HY-156087
    Cholicamideβ
    		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
  • HY-N10319R
    Artepillin C (Standard)
    		Inducer
    Artepillin C (Standard) is the analytical standard of Artepillin C (HY-N10319). This product is intended for research and analytical applications. 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 apoptosis, 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 (Standard)
  • HY-149052
    SZM-1209
    		Inhibitor
    SZM-1209 is an orally active, potent and specific RIPK1 inhibitor, with a Kd of 85 nM. SZM-1209 exhibits high anti-necroptotic activity (EC50=22.4 ± 8.1 nM). SZM-1209 shows anti-SIRS (systemic inflammatory response syndrome), and anti-ALI (acute lung injury) effects.
    SZM-1209
  • HY-151541
    MLKL-IN-3
    		Inhibitor
    MLKL-IN-3 (compound 66) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-3 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 31 nM. MLKL-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MLKL-IN-3
  • HY-N16764
    (rel)-Salcolin A
    		Inducer
    (rel)-Salcolin A is a flavonoid lignan compound with anticancer, anti-inflammatory, and neuroprotective activities. (rel)-Salcolin A has IC50 values ??of 66.69 μM and 56.12 μM against anaplastic thyroid carcinoma cells (HTH83) and papillary thyroid carcinoma cells (TPC1), respectively. (rel)-Salcolin A also inhibits LPS-induced NO production with an IC50 of 14.65 μM. (rel)-Salcolin A exerts its effects by inducing necroptosis in thyroid cancer cells, inhibiting the production of the inflammatory factor NO, and protecting against glutamate-induced neuronal cell damage, with a neuroprotective E50 of 47.44 μM. (rel)-Salcolin A can be used in research related to thyroid cancer, anti-inflammation, and neuroprotection. (rel)-Salcolin A can be naturally extracted from the leaves of Casearia arborea and the stems of Zea mays (corn).
    (rel)-Salcolin A
  • HY-173564
    DW34
    		Inhibitor
    DW34 is an orally active pan-BRD4-D1 biased inhibitor with additional BRD4-D2 inhibitive activity. DW34 displays comparable inhibitive efficacy to I-BET151 (HY-13235) (EC50 = 0.16 μM) with low nanomolar EC50 values of 0.14 μM. DW34 significantly reduces liver inflammation induced by LPS (HY-D1056) and APAP (HY-66005) via reducing chemokine expression and cellular necrosis.
    DW34
  • HY-163390
    RIP1 kinase inhibitor 9
    		Inhibitor
    RIP1 kinase inhibitor 9 (compound SY-1) is a selective RIP kinase inhibitor. RIP1 kinase inhibitor 9 effectively suppresses the central inflammatory response induced by epilepsy. RIP1 kinase inhibitor 9 inhibits Z-VAD-FMK (HY-16658B)-induced necroptosis in HT-29 cells with an EC50 of 7.04 nM.
    RIP1 kinase inhibitor 9
  • HY-183232
    SRS6-11
    		Inducer
    SRS6-11 is an iron death-independent necrotic cell death (Necrosis) inducer. SRS6-11 retains significant lethality in the presence of α-tocopherol (HY-W020044). SRS6-11 can be used in fibrosarcoma research.
    SRS6-11
  • HY-W144308R
    Tetrachlorohydroquinone (Standard)
    		Inducer
    Tetrachlorohydroquinone (Standard) is the analytical standard of Tetrachlorohydroquinone (HY-W144308). This product is intended for research and analytical applications. Tetrachlorohydroquinone (TCHQ) is a metabolite of Pentachlorophenol. Tetrachlorohydroquinone induces reactive oxidant stress (ROS), inhibits apoptosis and induces necrosis in primary mouse splenocytes. Tetrachlorohydroquinone increases DNA lesions and induces oxidative stress in rodents.
    Tetrachlorohydroquinone (Standard)
  • HY-W013699R
    Chlorhexidine diacetate (Standard)
    		Inducer
    Chlorhexidine diacetate (Standard) is the analytical standard of Chlorhexidine diacetate (HY-W013699). This product is intended for research and analytical applications. Chlorhexidine diacetate is a orally active cationic antimicrobial agent that targets microbial cell membranes. Chlorhexidine diacetate binds to cell membrane phospholipids non-specifically, destroys membrane structure and induces leakage of cell contents. Chlorhexidine diacetate has broad-spectrum bactericidal activity against both Gram-positive and Gram-negative bacteria. Chlorhexidine diacetate 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 diacetate (Standard)
  • HY-183538
    Necroptosis inducer 2
    		Inducer
    Necroptosis inducer 2 is a necroptosis inducer and copper chelator. Necroptosis inducer 2 chelates intracellular free copper ions, disrupts redox homeostasis, elevates ROS levels, disrupts mitochondrial membrane potential, and induces cancer cell necroptosis. Necroptosis inducer 2 upregulates the necroptosis markers p-MLKL and p-RIP3 expression. Necroptosis inducer 2 exhibits anti-tumor activity in mice. Necroptosis inducer 2 can be used for the research of cancer, such as triple-negative breast cancer.
    Necroptosis inducer 2
  • HY-162046
    Anticancer agent 178
    		Inducer
    Anticancer agent 178 (compound C2) is a potent anticancer agent. Anticancer agent 178 inhibits MDA-MB 231 cells proliferation and metabolic activity with IC50s of 1.1 and 4.2 μM. Anticancer agent 178 induces ferroptosis and necroptosis in cells.
    Anticancer agent 178
  • HY-168640
    RIP3 activator 1
    		Inducer
    RIP3 activator 1 (compound C8) is a potent RIP3 activator. RIP3 activator 1 inhibits cell growth. RIP3 activator 1 induces necroptosis through the RIP3/p62/Keap1 signaling pathway. RIP3 activator 1 increases the protein expression of p-MLKL. RIP3 activator 1 induces autophagy. RIP3 activator 1 increases accumulation of LC3-II and p62 protein expression.
    RIP3 activator 1
  • HY-183781
    RIPK1-IN-41
    		Inhibitor
    RIPK1-IN-41 is an orally active RIPK1 inhibitor with an IC50 of 92 nM and a KD of 106.8 nM. RIPK1-IN-41 reduces the phosphorylation level of RIPK1, inhibits necrosome formation, blocks the activation of RIPK3 and MLKL, maintains mitochondrial and lysosomal functions, preserves cell membrane integrity, and suppresses necroptosis. RIPK1-IN-41 alleviates hypothermia and multi-organ damage in a mouse model of systemic inflammatory response syndrome induced by mTNF-α. RIPK1-IN-41 is applicable to research related to systemic inflammatory response syndrome.
    RIPK1-IN-41
  • HY-176407
    ZYH-23
    		Inhibitor
    ZYH-23 is a potent necroptosis inhibitor. ZYH-23 blocks necroptosis by inhibiting RIPK1, RIPK3, and MLKL phosphorylation via HSP90 targeting.
    ZYH-23
  • HY-B1248A
    Chlorhexidine acetate hydrate
    		Inducer
    Chlorhexidine acetate hydrate is a orally active cationic antimicrobial agent that targets microbial cell membranes. Chlorhexidine acetate hydrate binds to cell membrane phospholipids non-specifically, destroys membrane structure and induces leakage of cell contents. Chlorhexidine acetate hydrate has broad-spectrum bactericidal activity against both Gram-positive and Gram-negative bacteria. Chlorhexidine acetate hydrate 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 acetate hydrate