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 (130):

By Effects:	Control (1) Inhibitors (52) Activators (4) Inducers (64)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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.

HY-149052

SZM-1209	Inhibitor
SZM-1209 is an orally active, potent and specific RIPK1 inhibitor, with a K_d 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.

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.

HY-W747676

Glyphosate-¹³C
Glyphosate-¹³C is the ¹³C-labeled Glyphosate (HY-B0863). Glyphosate, a non-selective systemic biocide with broad-spectrum activity, is an herbicidal derivative of the amino acid glycine. Glyphosate 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 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-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.

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.

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.

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).

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.

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.

HY-161343

HDL-16	Inhibitor	99.19%
HDL-16 is a potent P2Y₁₄R antagonist with an IC₅₀ of 0.3095 nM. HDL-16 ameliorates DSS (HY-116282C)-induced colitis through suppressing necroptosis of intestinal epithelium cells (IECs) and protecting mucosal barrier function.

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.

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).

HY-W319332

Necrostatin-21	Inhibitor
Necrostatin-21 (Compound Nec-21) is a necroptosis inhibitor with an EC₅₀ of 0.5 μM. Necrostatin-21 has a dual inhibitory effect on the RIP1 and JNK3 kinases. Necrostatin-21 can be used for the researches of infection, cardiovascular and neurological disease, such as Alzheimer disease .

HY-168623

EGFR-IN-134	Inducer
EGFR-IN-134 (compound 3f), a triazolo[3,4-a]isoquinoline derivative, is a potent EGFR inhibitor with an IC₅₀ of 0.023 µM. EGFR-IN-134 induces apoptosis and necrosis. EGFR-IN-134 initiates cell cycle arrest at the G2/M and pre-G1 phases, downregulates anti-apoptotic protein Bcl2 and upregulates pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. EGFR-IN-134 shows antiproliferative and anticancer activity.

HY-N11479

Vallesiachotamine	Inducer
Vallesiachotamine, a known monoterpene indole alkaloid, possesses anti-tumor activity.

HY-174820

AZ'320	Inhibitor
AZ'320 is an ATP-competitive necroptosis (EC₅₀ of 4.9 μM) inhibitor and a RIPK1 (pK_D of 5.45) inhibitor. AZ'320 inhibits necroptosis by inhibiting RIPK1 phosphorylation. AZ’320 prevents mortality of the mice and rescues temperature and body weight in SIRS mice models. AZ'320 can be used for researches of cancer and inflammation.

HY-161995

FGFR1/VEGFR2-IN-2	Activator
FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC₅₀ values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC₅₀ values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC₅₀ of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC₅₀ for MCF-7 cell line exceeds 100 µM, and the IC₅₀ for MDA-MB-231 is 69.17 µM, non-toxic to normal cells.

HY-W014839R

Cyclamic acid sodium (Standard)	Inducer
Cyclamic acid (sodium) (Standard) is the analytical standard of Cyclamic acid (sodium). This product is intended for research and analytical applications. Cyclamic acid (Cyclohexylsulfamic acid) sodium is one of the most widely used artificial sweetenersin food and pharmaceuticals.

HY-154861

Anticancer agent 118	Inducer
Anticancer agent 118, a N‑acylated ciprofloxacin derivative, has anti-bacterial and anticancer activities. Anticancer agent 118 shows high activity against Gram-positive strains and antiproliferative activities against prostate PC3 cells. Anticancer agent 118 can be used for antitumor research.

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