2. Signaling Pathways
  3. Immunology/Inflammation
  4. NOD-like Receptor (NLR)

NOD-like Receptor (NLR)

NOD-like Receptor (NLR)

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Nucleotide oligomerization domain (NOD)-like receptors (NLRs) are critical cytoplasmic pattern-recognition receptors (PRRs) that play an important role in the host innate immune response and immunity homeostasis. There are 23 NLR family members in humans and at least 34 NLR genes in mice. NLRs are expressed in many cell types including immune cells and epithelial cells, although certain NLR family members are expressed primarily in phagocytes including macrophages and neutrophils. The NLR family are most commonly classified according to their N-terminal domain, falling into one of four subfamilies; NLRA, NLRB, NLRC and NLRP.

The NLRs recognize various ligands from microbial pathogens (peptidoglycan, flagellin, viral RNA, fungal hyphae, etc.), host cells (ATPs, cholesterol crystals, uric acid, etc.), and environmental sources (alum, asbestos, silica, alloy particles, UV radiation, skin irritants, etc.). Most NLRs act as PRRs, recognizing the above ligands and activate inflammatory responses. However, some NLRs may not act as PRRs but instead respond to cytokines such as interferons. The activated NLRs show various functions that can be divided into four broad categories: inflammasome formation, signaling transduction, transcription activation, and autophagy.

NOD-like Receptor (NLR) Isoform Specific Products:

NOD-like Receptor (NLR) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-130494
    (±)11(12)-EET
    		Inhibitor 98.30%
    (±)11(12)-EET is a NLRP3 inflammasome inhibitor. (±)11(12)-EET can be used for the research of anti-inflammatory, angiogenic and cardioprotective.
    (±)11(12)-EET
  • HY-N0921
    Dihydromethysticin
    		Activator 99.94%
    Dihydromethysticin is an orally active natural active ingredient. Dihydromethysticin can be extracted from Piper methysticum. Dihydromethysticin inhibits carboxylesterase 1 (Ki = 68.2 μM) and CYP2A5. Dihydromethysticin upregulates NLRC3 and induces Apoptosis. Dihydromethysticin exhibits anticancer activity against colorectal cancer and lung adenoma.
    Dihydromethysticin
  • HY-144223
    NLRP3/AIM2-IN-2
    		99.93%
    NLRP3/aim2-in-2 (compound 8) is a new potent inhibitor with different species-specific effects on NLRP3 and AIM2 inflammasome dependent cell death. Its < b > IC < sub > 50 < / sub > < / b > value is 0.2392 μ M。
    NLRP3/AIM2-IN-2
  • HY-161834
    RG100204
    		Inhibitor 99.50%
    RG100204 is a selective, orally available inhibitor of the aquaporin AQP9. RG100204 directly inhibits AQP9 channel function, preventing the transmembrane transport of water, glycerol, and H2O2. RG100204 reduces the activation of the NLRP3 inflammasome and p38 MAPK signaling pathways, thereby alleviating inflammation and pyroptosis. RG100204 reduces multi-organ dysfunction in a mouse sepsis model and shows glucose-regulating effects in diabetic db/db mice.
    RG100204
  • HY-N0696
    Sipeimine
    		Inhibitor ≥98.0%
    Sipeimine (Imperialine) is an inhibitor targeting the PI3K/AKT/NF-κB pathway and NLRP3 inflammasome, which can competitively bind to PI3K and p65. Sipeimine inhibits PI3K/AKT phosphorylation, blocks NF-κB nuclear translocation and NLRP3 inflammasome activation. Sipeimine exerts anti-inflammatory activities, inhibits pyroptosis and ferroptosis, and protects the extracellular matrix. Sipeimine can reduce cartilage degradation and synovial inflammation in osteoarthritis and improve PM2.5-induced lung injury. Sipeimine is mainly used in the study of anti-inflammatory and degenerative diseases.
    Sipeimine
  • HY-156413
    NLRP3 agonist 1
    		Agonist 99.47%
    NLRP3 agonist 1 (compound 23) is a potent and orally active NLRP3 agonist. NLRP3 agonist 1 can activate the enzyme Caspase-1 to cleave pro-IL-1β and pro-IL-18 proinflammatory cytokines into their mature forms.
    NLRP3 agonist 1
  • HY-119684
    Maresin 2
    		Inhibitor
    Maresin 2 is an anti-inflammatory and pro-resolving mediator from human macrophages. Maresins are a new family of anti-inflammatory and pro-resolving lipid mediators biosynthesized from docosahexaenoic acid (DHA) by macrophages.
    Maresin 2
  • HY-158155
    CVN293
    		Inhibitor 99.91%
    CVN293 is a selective and brain permeable potassium ion (K+) channel KCNK13 inhibtor with IC50s of 41 nM and 28 nM for hKCNK13 and mKCNK13, respectively. CVN293 potently inhibits the NLRP3-inflammasome mediated production of the proinflammatory cytokine IL-1β in microglia.
    CVN293
  • HY-W082785A
    L6H21
    		Inhibitor 99.19%
    L6H21, a Chalcone (HY-121054) derivative, is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor. L6H21 directly binds to MD-2 protein with a high affinity and low KD value of 33.3 μM, blocking the formation of the LPS-TLR4/MD-2 complex. L6H21 inhibits LPS-induced expression of TNF-α and IL-6 in RAW264.7 macrophages, with IC50 values of 6.58 and 8.59 μM, respectively. L6H21 can be used for alcoholic liver disease, metabolic disturbance and neuroinflammation research.
    L6H21
  • HY-N1431
    Tabersonine
    		Inhibitor 98.14%
    Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.
    Tabersonine
  • HY-N0257
    Epimedin A
    		Inhibitor 99.43%
    Epimedin A, one of the main flavonoid active components in Herba Epimedii, is orally active. Epimedin A can inhibit osteoclastogenesis, differentiation, and bone resorption. Epimedin A also possesses anti-inflammatory activity. Epimedin A can be used in the research of osteoporosis and inflammatory diseases.
    Epimedin A
  • HY-N6051
    (-​)​-Maackiain
    		Activator 99.91%
    (-)-Maackiain is a pterocarpan phytoalexin produced from Sophora flavescens. (-)-Maackiain is toxic to several genera of fungal pathogens of legume and non legume hosts. (-)-Maackiain enhances the activation of NLRP3 inflammasome, inhibits the activation of NF-κB pathway, exhibiting thereby immunostimulatory and anti-inflammatory activities. (-)-Maackiain is orally active.
    (-​)​-Maackiain
  • HY-120007
    JC124
    		Inhibitor 99.72%
    JC124 is a specific NLRP3 inflammasome inhibitor. JC124 has anti-inflammatory and neuroprotective effects.
    JC124
  • HY-149478
    JT002
    		Inhibitor 99.54%
    JT002 is an orally active and selective NLRP3 inflammasome assembly inhibitor. JT002 reduces NLRP3-dependent proinflammatory cytokine (such as IL-1β, IL-1α, IL-18) production and pyroptosis. JT002 blocks NLRP3 inflammasome complex formation. JT002 reduces airway hyperresponsiveness and airway neutrophilia in mice. JT002 can be used for the study of a variety of inflammatory diseases, such as Muckle-Wells syndrome (MWS).
    JT002
  • HY-150206
    NLRP3-IN-13
    		Inhibitor 98.03%
    NLRP3-IN-13 (Compound C77 in reference patent) is a selective and potent NLRP3 inhibitor (IC50: 2.1 μM). NLRP3-IN-13 inhibits NLRP3 andNLRC4 inflammasomes, and inhibits NLRP3-mediated IL-1β production. NLRP3-IN-13 also inhibits NLRP3 ATPase activity. NLRP3-IN-13 can be used in the research of neuroinflammatory disorders.
    NLRP3-IN-13
  • HY-162877
    AZD4144
    		Inhibitor 99.67%
    AZD4144 is an orally active NLRP3 inhibitor (EC50: 0.082 μM). AZD4144 effectively inhibits the release of IL-1β when NLRP3 is overactivated, exerting an anti-inflammatory effect. AZD4144 has low inhibitory effect on hERG and low cardiotoxicity. AZD4144 has the potential to study diseases and conditions associated with NLRP3 inflammasome activation.
    AZD4144
  • HY-P99555
    Tomaralimab
    		Inhibitor
    Tomaralimab (OPN-305) is a humanized anti-TLR2 IgG4 monoclonal antibody. Tomaralimab inhibits TLR2, MyD88, NLRP3, and reduces pro-inflammatory cytokine (IL-1β, IL-6, IL-8) production. Tomaralimab reduces tau pathology. Tomaralimab improves cognition, atopic dermatitis. Tomaralimab has anticancer effects on pancreatic ductal adenocarcinoma. Tomaralimab is being studied in myelodysplastic syndrome (MDS), atopic dermatitis, pancreatic ductal adenocarcinoma, Alzheimer's disease, and myocardial ischemia/reperfusion injury.
    Tomaralimab
  • HY-158024
    NDT-19795
    		Inhibitor 99.16%
    NDT-19795 is an effective inhibitor of the NLRP3 inflammasome with an IC50 value of 66 nM in the PBMC method and 4.7 μM in the WB method. NDT-19795 is a carboxylic acid-active substance that can be converted from NT-0796 (HY-156438) within cells. NDT-19795 can be used for the study of neurological diseases.
    NDT-19795
  • HY-137245
    Emlenoflast
    		Inhibitor 98.19%
    Emlenoflast (MCC7840), a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM. Emlenoflast can be used for the research of inflammatory diseases.
    Emlenoflast
  • HY-101868
    INF39
    		Inhibitor 99.86%
    INF39 is an irreversible and noncytotoxic NLRP3 inhibitor.
    INF39
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
NOD-like Receptor (NLR) Isoform Comparison

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