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 관련 제품 (165):

By Effects:	Inhibitors (64) Control (1) Activators (4) Inducers (83)

Cat. No.	상품명	효과	Purity	Chemical Structure

HY-181944

RIPK1-IN-40	Inhibitor
RIPK1-IN-40 (Compound 51) is a RIPK1 inhibitor and anti-necroptotic agent (with an EC₅₀ of 0.07 μM against necroptosis). RIPK1-IN-40 binds to the kinase domain of RIPK1, forms hydrogen bond interactions with Met95, and establishes additional polar contacts with Asp156 to stabilize binding, thereby inhibiting necroptosis. RIPK1-IN-40 can be used for the research of colorectal cancer.

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-W010201S1

Citronellol-d₃
Citronellol-d₃ ( (±)-Citronelloll-d₃) is the deuterium labeled Citronellol (HY-W010201). Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.

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-P5142

ω-Hexatoxin-Hv1a	Inhibitor
ω-Hexatoxin-Hv1a (ω-ACTX-Hv1; ω-Atracotoxin-HV1) is an orally active insecticidal neurotoxin containing an inhibitor cystine knot motif and a selective calcium channel inhibitor. ω-Hexatoxin-Hv1a blocks L-type voltage-dependent Ca²⁺ channels and reduces intracellular calcium ion concentration, thereby decreasing apoptosis, necroptosis and oxidative stress, and promoting cell recovery and energy level elevation. ω-Hexatoxin-Hv1a causes larval paralysis and death by impairing neurotransmission in the central nervous system of insects. It shows high injectable toxicity against insects of multiple orders, but exhibits weak oral toxicity. ω-Hexatoxin-Hv1a is widely applicable to studies related to ischemia-reperfusion injury, atopic dermatitis, and ischemic injury of cardiomyocytes and neurons.

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-B1218S

Sulfaphenazole-d₄		99.66%
Sulfaphenazole-d₄ is the deuterium labeled Sulfaphenazole (HY-B1218). Sulfaphenazole is a selective inhibitor of human cytochrome P450 (CYP) 2C9 enzyme. Sulfaphenazole is a cytoprotective agent against light-induced death of photoreceptors. Sulfaphenazole inhibits light-induced necrosis and mitochondrial stress-initiated apoptosis. Sulfaphenazole is an off patent sulfonamide antibiotic and demonstrates bactericidal activity through enhanced M1 macrophage activity. Sulfaphenazole can significantly reduce infarct size and restore post-ischemic coronary flow following ischemia and reperfusion.

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-129577

Aplysin	Inhibitor
Aplysin is a brominated sesquiterpene with an isoprene backbone that exhibits hepatoprotective, immunomodulatory, and antitumor activities. Aplysin effectively prevents spontaneous pancreatic necrosis and inflammatory responses in NOD mice.

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-121382R

Gypsogenin (Standard)	Inducer
Cinosulfuron (Standard) is the analytical standard of Cinosulfuron. This product is intended for research and analytical applications. Gypsogenin is a selective mixed-type BChE inhibitor (K_i=19.99 μM) that also exhibits significant cytotoxicity against various human cancer cell lines. Gypsogenin inhibits tumor growth by inducing cell cycle arrest and triggering apoptosis. Gypsogenin displays antibacterial activity against bacteria such as Bacillus subtilis and Bacillus thuringiensis, and often serves as a key parent nucleus for the synthesis of anticancer compounds. Gypsogenin is widely used in research on Alzheimer's disease and various cancers including colon cancer, melanoma, and leukemia.

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-181093

EGFR-IN-191	Inducer
EGFR-IN-191 is an anti-tumor agent targeting both EGFR and AKT. EGFR-IN-191 exerts its anti-tumor activity by inducing DNA damage, apoptosis, cell cycle arrest, and inhibition of the PI3K/AKT-EGFR signaling pathway in tumor cells. EGFR-IN-191 can be used in the study of tumors such as triple-negative breast cancer.

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.

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