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-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.

HY-155146

Anticancer agent 146	Inducer
Anticancer agent 146 (compound 1.19) is a necroptosis inducer. Anticancer agent 146 has anti-tumor efficacy in the mouse MDA-MB-231 xenograft model.

HY-W004702S

Methyl methanesulfonate-d₃	Inducer
Methyl methanesulfonate-d₃ is the deuterium labeled Methyl methanesulfonate (HY-W004702). Methyl methanesulfonate is an alkylating agent which transfers methyl groups, and induces DNA damage. Methyl methanesulfonate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.

HY-162348

Antitumor agent-145	Inhibitor
Antitumor agent-145 (Compound Ir5) is a tumor inhibitor with remarkable fluorescence and mitochondrial targeting, which exerts anti-cancer effects by inducing necroptosis and activating the necroptosis-related immune response.

HY-147521

Antitumor photosensitizer-3
Antitumor photosensitizer-3 (Compound I) is a chlorin derivative. Antitumor photosensitizer-3 induces tumor cells apoptosis and necrosis under 650 nm laser irradiation. Antitumor photosensitizer-3 exhibits lower skin photo-toxicity than positive reference m-THPC in vivo.

HY-149080

Antiparasitic agent-16	Inducer
Antiparasitic agent-16, a pyridine-thiazolidinone, has anti-Trypanosoma cruzi and leishmanicidal activities. Antiparasitic agent-16 has IC₅₀s of 1.0 μM and 0.6 μM against trypomastigote and amastigote forms of T. cruzi. Antiparasitic agent-16 has IC₅₀s of 150.2 μM and 16.75 μM against trypomastigote and amastigote forms of L. amazonensis. Antiparasitic agent-16 induces parasite cell death through necrosis induction. Antiparasitic agent-16 induces morphological changes such as shortening, retraction and curvature of the parasite body and leakage of internal content with T. cruzi trypomastigotes.

HY-161911

Necroptosis-IN-5	Inhibitor
Necroptosis-IN-5 (Compound 26) is an orally active necroptosis inhibitor. Necroptosis-IN-5 also exhibits potent inhibitory activity against receptor-interacting protein kinase 1 (RIPK1). Necroptosis-IN-5 can be used to study necroptosis-related inflammatory diseases, neurodegenerative diseases, and cancers.

HY-178380

HDAC8-IN-14	Activator
HDAC8-IN-14, a curcuminoid derivative, is a selective HDAC8 inhibitor with a Ki of 9 nM. HDAC8-IN-14 induces the production of reactive oxygen species (ROS), disrupts mitochondrial membrane potential, and promotes apoptosis. HDAC8-IN-14 can significantly promote the accumulation of cells in the sub-G0/G1 phase, consistent with apoptotic or necrotic cell death. HDAC8-IN-14 induces upregulation of cytochrome c, cleaved caspase-3, and the pro-apoptotic protein Bak while leaving the anti-apoptotic Bcl-2 levels unaltered. HDAC8-IN-14 can be used for the study of leukemia.

HY-178762S

RIPK1-IN-35	Inhibitor
RIPK1-IN-35 is a selective and orally active RIPK1 inhibitor with an IC₅₀ of 5.33 nM. RIPK1-IN-35 has a potent protective effect against necroptosis in both human and murine cells. RIPK1-IN-35 shows good therapeutic effects in both TNF-α-induced systemic inflammatory response syndrome and DSS (HY-116282C)-induced inflammatory bowel disease models. RIPK1-IN-35 can be used to the study of inflammatory diseases related to necroptosis.

HY-162569

Ru-TRZ2	Inducer
Ru-TRZ2 is a potent ruthenium-based chemotherapeutic agent. Ru-TRZ2 induces apoptosis and necroptosis. Ru-TRZ2 shows antitumor activity.

HY-151542

MLKL-IN-4	Inhibitor
MLKL-IN-4 (compound 56) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-4 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC₅₀ of 82 nM. MLKL-IN-4 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-N8380

(-)-Latifolin	Inducer
(-)-Latifolin, a flavonoid, induces apoptotic cell death by targeting PI3K/AKT/mTOR/p70S6K signaling. (-)-Latifolin significantly inhibits the cell proliferation of oral squamous cell carcinoma (OSCC), and causes the anti-metastatic activities by effectively blocking cell migration, invasion, and adhesion via the inactivation of FAK/Src. (-)-Latifolin suppresses autophagic-related proteins and autophagosome formation. (-)-Latifolin inhibits necroptosis by dephosphorylating necroptosis-regulatory proteins (RIP1, RIP3, and MLKL). (-)-Latifolin has beneficial effects on anti-aging, anti-carcinogenic, anti-inflammatory, and cardio-protective activities.

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