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):

By Effects:	Control (1) Inhibitors (46) Activators (3) Inducers (59)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-155146

Anticancer agent 146	Inducer
Anticancer agent 146 (compound 1.19) is a necroptosis inducer. Anticancer agent 146 has anti-tumor efficacy in the mouse MDA-MB-231 xenograft model.

HY-162348

Antitumor agent-145	Inhibitor
Antitumor agent-145 (Compound Ir5) is a tumor inhibitor with remarkable fluorescence and mitochondrial targeting, which exerts anti-cancer effects by inducing necroptosis and activating the necroptosis-related immune response.

HY-147521

Antitumor photosensitizer-3
Antitumor photosensitizer-3 (Compound I) is a chlorin derivative. Antitumor photosensitizer-3 induces tumor cells apoptosis and necrosis under 650 nm laser irradiation. Antitumor photosensitizer-3 exhibits lower skin photo-toxicity than positive reference m-THPC in vivo.

HY-149080

Antiparasitic agent-16	Inducer
Antiparasitic agent-16, a pyridine-thiazolidinone, has anti-Trypanosoma cruzi and leishmanicidal activities. Antiparasitic agent-16 has IC₅₀s of 1.0 μM and 0.6 μM against trypomastigote and amastigote forms of T. cruzi. Antiparasitic agent-16 has IC₅₀s of 150.2 μM and 16.75 μM against trypomastigote and amastigote forms of L. amazonensis. Antiparasitic agent-16 induces parasite cell death through necrosis induction. Antiparasitic agent-16 induces morphological changes such as shortening, retraction and curvature of the parasite body and leakage of internal content with T. cruzi trypomastigotes.

HY-161911

Necroptosis-IN-5	Inhibitor
Necroptosis-IN-5 (Compound 26) is an orally active necroptosis inhibitor. Necroptosis-IN-5 also exhibits potent inhibitory activity against receptor-interacting protein kinase 1 (RIPK1). Necroptosis-IN-5 can be used to study necroptosis-related inflammatory diseases, neurodegenerative diseases, and cancers.

HY-162569

Ru-TRZ2	Inducer
Ru-TRZ2 is a potent ruthenium-based chemotherapeutic agent. Ru-TRZ2 induces apoptosis and necroptosis. Ru-TRZ2 shows antitumor activity.

HY-151542

MLKL-IN-4	Inhibitor
MLKL-IN-4 (compound 56) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-4 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC₅₀ of 82 nM. MLKL-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-N8380

(-)-Latifolin	Inducer
(-)-Latifolin, a flavonoid, induces apoptotic cell death by targeting PI3K/AKT/mTOR/p70S6K signaling. (-)-Latifolin significantly inhibits the cell proliferation of oral squamous cell carcinoma (OSCC), and causes the anti-metastatic activities by effectively blocking cell migration, invasion, and adhesion via the inactivation of FAK/Src. (-)-Latifolin suppresses autophagic-related proteins and autophagosome formation. (-)-Latifolin inhibits necroptosis by dephosphorylating necroptosis-regulatory proteins (RIP1, RIP3, and MLKL). (-)-Latifolin has beneficial effects on anti-aging, anti-carcinogenic, anti-inflammatory, and cardio-protective activities.

HY-B1248R

Chlorhexidine (Standard)	Inducer
Chlorhexidine (Standard) is the analytical standard of Chlorhexidine (HY-B1248). This product is intended for research and analytical applications. Chlorhexidine is a orally active cationic antimicrobial agent that targets microbial cell membranes. Chlorhexidine binds to cell membrane phospholipids non-specifically, destroys membrane structure and induces leakage of cell contents. Chlorhexidine has broad-spectrum bactericidal activity against both Gram-positive and Gram-negative bacteria. Chlorhexidine 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).

HY-130369

NSC10010 hydrochloride	Inducer
NSC10010 hydrochloride inhibits gammaherpesvirus associated B-lymphomas growth through activation of NF-kB and c-Myc-mediated signaling pathways. NSC10010 hydrochloride induces necrotic cell death in gammaherpesvirus infected B-cells. NSC10010 hydrochloride is also an inhibitor of Mtb ClpC1 ATPase.

HY-B1145R

Chlorhexidine dihydrochloride (Standard)	Inducer
Chlorhexidine dihydrochloride (Standard) is the analytical standard of Chlorhexidine dihydrochloride (HY-B1145). This product is intended for research and analytical applications. 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).

HY-121261

Antineoplastic agent-1	Inducer
Antineoplastic agent-1 is an alkylating agent and a genotoxic agent that can induce DNA damage. Antineoplastic agent-1 can lead to irreversible damage and progressive death of liver cells due to necroptosis and apoptosis. Antineoplastic agent-1 can cause alkylation damage to hematopoietic cells and stromal cells in the bone marrow. Antineoplastic agent-1 can be used in tumor research.

HY-B1984R

p,p'-DDD (Standard)	Inducer
p,p'-DDD (Standard) is the analytical standard of p,p'-DDD (HY-B1984) . This product is intended for research and analytical applications. p,p'-DDD (4,4’-DDD) is an organochlorine insecticide, a major metabolite of p,p'-DDT. p,p'-DDD is an agonist at estrogen receptor α(ERα) and ERβ. p,p'-DDD increases DNA damage, apoptosis and necrosis in peripheral blood. p,p'-DDD stimulates cell proliferation in SKBR3 cells. p,p'-DDD activates the AP-1 transcription factor. p,p'-DDD decreases sleep times of barbiturates and steroids in rats.

HY-W014839S

Cyclamic acid-d₁₁ sodium	Inducer
Cyclamic acid-d₁₁ (Sodium cyclamate-d₁₁) sodiumis deuterium labeled Cyclamic acid (sodium). Cyclamic acid sodium (Sodium cyclamate) is a commonly used sweetener. Cyclamic acid sodium is toxic to osteoblasts and can inhibit cell proliferation, induce apoptosis and reduce cell mineralization. Cyclamic acid sodium causes focal necrosis of bladder organs in rats in vitro, which can promote bladder cancer, but some studies have shown that low doses of Cyclamic acid sodium have no carcinogenic effect. In addition, Cyclamic acid sodium has no effect on insulin and glucagon secretion induced by arginine.

HY-B0863B

Glyphosate isopropylammonium	Inducer
Glyphosate isopropylammonium, a non-selective systemic biocide with broad-spectrum activity, is an herbicidal derivative of the amino acid glycine. Glyphosate isopropylammonium inhibits the enzymatic activity of the 5-endopyruvylshikimate 3-phosphate synthase (EPSPS) in the shikimic acid pathway, preventing the synthesis of the aromatic amino acids tyrosine, phenylalanine, and tryptophan. Glyphosate isopropylammonium induces oxidative stress, neuroinflammation, and mitochondrial dysfunction, processes that lead to neuronal death by autophagia, necrosis, or apoptosis, as well as the appearance of behavioral and motor disorders.

HY-14909R

Bardoxolone (Standard)	Inhibitor
Bardoxolone (Standard) is the analytical standard of Bardoxolone (HY-14909). This product is intended for research and analytical applications. Bardoxolone is an orally active activator of nuclear regulatory factor (NRf-2) and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone inhibits SARS-CoV-2 3CL protease with an EC₅₀ value of 0.43 μM in vero cells. Bardoxolone also inhibits necroptosis in HT-29 cells with an EC₅₀ value of 1.30 μM by blocking necrosome formation through inhibiting phosphorylation of RIPK1 and RIPK3. Bardoxolone can be used in research on COVID-19, TNF-induced systemic inflammatory response syndrome (SIRS), and cerebral ischemia-reperfusion injury.

HY-129577

Aplysin	Inhibitor
Aplysin is a brominated sesquiterpene with an isoprene backbone that exhibits hepatoprotective, immunomodulatory, and antitumor activities. Aplysin effectively prevents spontaneous pancreatic necrosis and inflammatory responses in NOD mice.

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