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 (49):

By Effects:	Inhibitors (25) Activator (1) Inducers (19)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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-163092

LEI-515	Inhibitor
LEI-515 is a first-in-class peripherally restricted, reversible MAGL inhibitor. LEI-515 increases 2-AG levels in peripheral organs, but not mouse brain. LEI-515 attenuated liver necrosis, oxidative stress and inflammation in a CCl4-induced acute liver injury model.

HY-162377

HDAC-IN-70	Inducer
HDAC-IN-70 (compound 4c) is HDAC6 inhibitor with the IC₅₀ values of 64.13 nM, 166 nM, 618 nM and 253 nM for HDAC6, HDAC1, HDAC2 and HDAC4, respectively. HDAC-IN-70 induces cell cycle arrest, apoptosis and necrotic. HDAC-IN-70 can be used for study of leukemia.

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-156119

MLKL-IN-6	Inhibitor
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-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.

HY-P5557

TP4 (Nile tilapia piscidin)	Inducer
TP4 (Nile tilapia piscidin) is an orally active piscidin-like antimicrobial peptide. TP4 inhibits multiple gram positive and negative strains (MIC: 0.03-10 μg/mL). TP4 shows hemolytic activities. TP4 enhances immune response, antioxidant activity, and intestinal health against bacterial infections. TP4 also has anti-tumor effect, and induces necrosis by triggering mitochondrial dysfunction in cancer cells.

HY-156087

Cholicamideβ	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-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-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-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-161343

HDL-16	Inhibitor
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-N11479

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

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.

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