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-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-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.

HY-149079

Antiparasitic agent-15	Inducer
Antiparasitic agent-15, a pyridine-thiazolidinone, has anti-Trypanosoma cruzi and leishmanicidal activities. Antiparasitic agent-15 has IC₅₀s of 0.9 μM and 0.64 μM against trypomastigote and amastigote forms of T. cruzi. Antiparasitic agent-15 has IC₅₀s of 42.2 μM and 9.58 μM against trypomastigote and amastigote forms of L. amazonensis. Antiparasitic agent-15 induces parasite cell death through necrosis induction. Antiparasitic agent-15 induces morphological changes such as shortening, retraction and curvature of the parasite body and leakage of internal content with T. cruzi trypomastigotes.

HY-157963

RIPK1-IN-23	Inhibitor
RIPK1-IN-23 (compound 19) is a RIPK1 inhibitor with potent anti-necroptotic effects in HT-29 cells (EC₅₀ of 1.7 nM). RIPK1-IN-23 shows anti-inflammatory activities.

HY-120600

Sibiriline	Inhibitor
Sibiriline is a specific competitive inhibitor of RIPK1 that targets the RIPK1 ATP-binding site and locks it in an inactive conformation. Sibiriline inhibits TNF-induced RIPK1-dependent necroptosis and RIPK1-dependent apoptosis, but does not protect cells from caspase-dependent apoptosis. Sibiriline protects mice from concanavalin A-induced hepatitis and has the potential to inhibit immune-dependent hepatitis..

HY-161843

Necroptosis-IN-4	Inhibitor
Necroptosis-IN-4, a potent necroptosis inhibitor, is a RIP kinase 1 (RIPK1) inhibitor. Necroptosis-IN-4 has no inhibitory activity against RIPK3 and weak inhibitory activity against VEGFR1/2 and PDGFR-α.

HY-W738281

Chlorhexidine-d₈	Inducer
Chlorhexidine-d₈ is deuterium-labeled Chlorhexidine (HY-B1248). 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-160169A

Necrosis inhibitor 2 (hydrocholide)	Inhibitor
Necrosis inhibitor 2 hydrocholide (Compound B19) is a cell necrosis inhibitor. Necrosis inhibitor 2 hydrocholide can be used to study diseases related to the necrosis pathway, including inflammation, tumors, metabolic diseases and neurodegenerative diseases.

HY-173075

Anticancer agent 267	Inducer
Anticancer agent 267 (Compound 5q) is the activator for RIPK3 and MLKL. Anticancer agent 267 inhibits the proliferation in a variety of cancer cell lines (IC₅₀ for MDA-MB-231, MDA-MB-486 and MCF-7 is 9.79, 10.77 and 5.94 μM, respectively), arrests cell cycle at subG1 phase, and induces necroptosis in cell MDA-MB-231. Anticancer agent 267 exhibits antitumor activity in mouse xenograft models.

HY-W144308

Tetrachlorohydroquinone	Inducer	98.45%
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-163740

VEGFR-2-IN-46	Inducer
VEGFR-2-IN-46 (compound 4d) is a potent VEGFR-2 inhibitor with an EC₅₀ value of 67.0 nM. VEGFR-2-IN-46 shows cytotoxicity and induces cell cycle arrest at the G2/M phase. VEGFR-2-IN-46 induces necrosis and apoptosis.

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