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 (103):

By Effects:	Control (1) Inhibitors (38) Activators (3) Inducers (55)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-B0863S2

Glyphosate-d₂-1	Inducer
Glyphosate-d₂-1 is the deuterium labeled Glyphosate[1]. 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[2].

HY-W010800A

Cholesterol hemisuccinate Tris salt	Inhibitor	≥98.0%
Cholesterol hemisuccinate Tris salt (CHS-Tris) is a with hepatoprotective an anticancer activity. Cholesterol hemisuccinate Tris salt inhibits Acetaminophen (AAP, HY-66005) hepatotoxicity, and prevents AAP-induced hepatic apoptosis and necrosis. Cholesterol hemisuccinate Tris salt inhibits DNA polymerase and DNA topoisomerase to inhibit DNA replication and repair and cell division. Thus, Cholesterol hemisuccinate Tris salt inhibits tumor growth.

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[1].

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.

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.

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.

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.

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.

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.

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.

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).

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).

HY-B1984S

p,p'-DDD-d₈	Inducer
p,p'-DDD-d₈ is the deuterium labeled p,p'-DDD[1]. 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-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.

HY-N10520

Pectic acid	Inducer
Pectic acid (Methyl protopectin), a polygalacturonic acid, induces cell apoptosis and necrosis in pituitary tumor cells. Pectic acid can be used in the research of cancers and autoimmune disease.

HY-144277

RIPK1-IN-12	Inhibitor
RIPK1-IN-12 is a potent RIPK1 inhibitor. RIPK1-IN-12 inhibits necroptosis in both human and mouse cells, with EC₅₀ values of 1.6 and 2.9 nM, respectively.

HY-160170

Necrosis inhibitor 3	Inhibitor
Necrosis inhibitor 3 (compound B3) is a poteng inhibitor of necrosis, with the IC₅₀ value of 0.29 nM in HT29 cells.

HY-116107

AG311	Inducer
AG311 is an anticancer and antimetastatic agent. AG311 induces rapid necrosis in numerous cancer cell lines.

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.

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.

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