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 (71):

By Effects:	Inhibitors (30) Activators (3) Inducers (32)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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.

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.

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.

HY-156119

MLKL-IN-6	Inhibitor	98.57%
MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor targeting Mixed Lineage Kinase domain-like (MLKL). MLKL-IN-6 inhibits cell necrosis. MLKL-IN-6 inhibits MLKL phosphorylation and oligomerization during cell necrosis, inhibits immune cell death, and reduces the expression of adhesion factors. MLKL-IN-6 has low cytotoxicity, and it inhibits hepatic stellate cell activation, reduces liver fibrosis marker levels, and has anti-fibrotic effects.

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-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-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-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-164388

Z-VAD	Inducer
Z-VAD is a competitive, irreversible pan-caspase inhibitor. Z-VAD inhibits all 10 caspases, except for caspase-2 which is only weakly inhibited. Z-VAD decreases radiation-induced apoptosis. Z-VAD induces both autophagy and necrosis in irradiated MDA-MB-231 and H460 mouse xenografts. Z-VAD with radiation produces a significant tumor growth delay and shows dramatic antiangiogenic effect in cancer xenograft.

HY-W010800A

Cholesterol hemisuccinate Tris salt	Inhibitor
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-B0863S3

Glyphosate-¹³C₂,¹⁵N	Inducer
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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