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-152670
    JC2-11
    		Inhibitor 98.03%
    JC2-11 is an inhibitor of inflammatory corpuscles. JC2-11 inhibits domain-containing protein NLRC 4, absent in melanoma 2 (AIM 2) and non-canonical (NC) inflammatory corpuscles. JC2-11 reduces the secretion of caspase-1 (p20), the cleavage of gasdermin D (GSDMD), and the releases of IL-1β and lactate dehydrogenases (LDH) in inflammatory bodies. JC2-11 inhibits the activation of inflammatory bodies by destroying the production of reactive oxygen species and the activity of caspase-1.
    JC2-11
  • HY-N7400
    Phaseoloidin
    		99.92%
    Phaseoloidin is an orally active multi-target inhibitor. Phaseoloidin inhibits the activation of the NLRP3 inflammasome and blocks the caspase-11-GSDMD pyroptosis axis. Phaseoloidin reduces the expression of collagen-degrading enzymes to maintain the integrity of cartilage matrix. Phaseoloidin activates the AMPK/mTOR pathway to enhance autophagic function. Phaseoloidin exerts adverse effects on the growth and development of Manduca sexta and Spodoptera littoralis larvae, inhibits larval growth, and thereby helps Nicotiana attenuata defend against lepidopteran herbivorous insects. Phaseoloidin is applicable to research related to acute gouty arthritis and pulmonary fibrosis.
    Phaseoloidin
  • HY-P10227
    Xelafaslatide
    		Inhibitor 99.88%
    Xelafaslatide (ONL-1204) is a Fas receptor antagonist. Xelafaslatide blocks the Fas receptor signaling pathway and inhibits downstream apoptosis and inflammatory pathways. Xelafaslatide suppresses neuroinflammation and microglial activation in glaucoma models, protects retinal ganglion cells and prevents axonal degeneration. Xelafaslatide is applicable to relevant research on glaucoma.
    Xelafaslatide
  • HY-P5522A
    TriDAP dihydrochloride
    		Activator 99.16%
    TriDAP dihydrochloride (L-Ala-γ-D-Glu-meso-diaminopimelic acid dihydrochloride) is a NOD1 agonist with a Kd value of 34.5 μM. TriDAP dihydrochloride enhances the binding of NOD1-RICK, promotes RICK phosphorylation, and activates the NF-κB, TAK1, MEK/ERK, p38 and interferon response pathways. TriDAP dihydrochloride downregulates Runx2 via increasing ubiquitination and reduces trabecular bone parameters. TriDAP dihydrochloride decreases IκBα levels and increases p65 levels. TriDAP dihydrochloride induces the secretion of proinflammatory mediators IL-8 and prostaglandins, triggers tissue inflammation and innate immune activation, and inhibits SARS-CoV-2 replication in lung epithelial cells. TriDAP dihydrochloride increases the RANKL/OPG ratio in mice, reduces bone mass and enhances osteoclast activity, and inhibits new bone formation by decreasing the mineralization deposition rate in mice. TriDAP dihydrochloride can be used in research related to pulpitis, chronic ulcerative colitis, Crohn's disease and SARS-CoV-2 infection.
    TriDAP dihydrochloride
  • HY-W746708
    FK-565
    		Ligand 99.88%
    FK-565 is a nucleotide oligomerization domain-1 (NOD1) ligand. FK-565 induces murine model with arteritis.
    FK-565
  • HY-119684
    Maresin 2
    		Inhibitor
    Maresin 2 is an anti-inflammatory and pro-resolving mediator. Maresin 2 drives intestinal epithelial cell migration by activating the focal cell-matrix adhesion signaling pathway in primary human intestinal epithelial cells, thereby promoting mucosal wound repair. Maresin 2 alleviates nociceptive and anxiety-like behaviors in rats with type 1 diabetes by inhibiting IL-1β in the spinal cord and prefrontal cortex. Maresin 2 attenuates allergic airway inflammation in mice by inhibiting the activation of the NLRP3 inflammasome, Th2-type immune responses, and oxidative stress. Maresin 2 inhibits inflammatory and neuropathic trigeminal neuralgia and reduces neuronal activation in the trigeminal ganglion. Maresin 2 promotes inflammation resolution and mucosal repair after DSS-induced colitis or biopsy-induced colonic mucosal injury.
    Maresin 2
  • HY-78263
    MNS
    		99.55%
    MNS (NSC 170724), the beta-nitrostyrene derivative, is an orally active tyrosine kinase inhibitor, a broad-spectrum antiplatelet agent, and a PANoptosis inhibitor. MNS inhibits Src, Syk, and FAK with IC50 of 27.3, 2.8, and 97.6 μM, respectively. MNS inhibits NLRP3 inflammasome and β1 integrin. MNS completely inhibits U46619, ADP-, arachidonic acid-, collagen-, and thrombin-induced platelet aggregation with IC50 values of 2.1, 4.1, 5.8, 7.0, and 12.7 μM, respectively. MNS is cytotoxic to a variety of cells.
    MNS
  • HY-148258
    GDC-2394
    		Inhibitor 99.87%
    GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC50s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation. GDC-2394 could be used to study gouty arthritis.
    GDC-2394
  • HY-137888A
    Oxidized ATP trisodium salt
    		Inhibitor 98.0%
    Oxidized ATP (oATP) trisodium salt is a broad-spectrum P2 receptor inhibitor. Oxidized ATP trisodium salt irreversibly antagonizes P2X7R activation. Oxidized ATP trisodium salt inhibits c-reactive protein (CRP)-induced NLRP3 inflammasome activation. Oxidized ATP trisodium salt can be used for research of atherosclerosis.
    Oxidized ATP trisodium salt
  • 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-156413
    NLRP3 agonist 1
    		Agonist 99.47%
    NLRP3 agonist 1 (Compound 23) is an 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-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 studies of inflammation and neurological diseases.
    NDT-19795
  • 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-N1939
    Icariside I
    		Agonist 99.30%
    Icariside I (GH01) is an orally active metabolite of icalin. Icariside I improves estrogen deficiency-induced osteoporosis by simultaneously regulating osteoblast and osteoclast differentiation. Icariside I promotes ATP (HY-B2176) or Nigericin (HY-127019)-induced mtROS production and NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Icariside I does not alter the activation of NLRC4 and AIM2 inflammasomes. Icariside I inhibits breast cancer proliferation, apoptosis, invasion, and metastasis by targeting the IL-6/STAT3 pathway. Icariside I is a kynurenine-AhR pathway inhibitor that alleviates cancer by blocking tumor immune escape.
    Icariside I
  • HY-N0442
    5-O-Methylvisammioside
    		Inhibitor 99.90%
    5-O-Methylvisammioside (4'-O-β-D-Glucosyl-5-O-methylvisamminol) is an orally active natural chromone glycoside and multiple biological activities. 5-O-Methylvisammioside inhibits ferroptosis by activating the Nrf2/HO-1 signaling axis. 5-O-Methylvisammioside alleviates intestinal barrier damage by inhibiting the ROS/NF-κB/NLRP3 pathway. 5-O-Methylvisammioside exerts a protective effect against acute liver injury by reducing ALT/AST, decreasing inflammatory infiltration, and inhibiting IκB-α phosphorylation and NF-κB nuclear translocation. 5-O-Methylvisammioside blocks the HMGB1/RAGE/MEK/ERK signaling axis to exert anti-tumor and anti-angiogenic effects. 5-O-Methylvisammioside improves depression-like behaviors by inhibiting Src kinase and the NF-κB pathway.
    5-O-Methylvisammioside
  • HY-N0381
    Maackiain
    		Activator 99.83%
    Maackiain (DL-Maackiain) is an orally active multi-target inhibitor with anti-tumor activity and neuroprotective effects. Maackiain activates the AMPK, NLRP3 and Nrf2/HO-1 pathways, and inhibits key targets such as NF-κB, mTOR, MAO-B, NFATc1 and PKCδ, thereby precisely regulating processes including apoptosis, autophagy and pyroptosis. Maackiain also effectively inhibits microglial activation, osteoclast formation, and proliferation and invasion of tumor cells, and protects dopaminergic neurons from damage. Maackiain is applicable to the research of various diseases such as Alzheimer's disease, osteoporosis, sepsis and dengue fever。
    Maackiain
  • HY-117878
    ML345
    		Inhibitor 99.37%
    ML345 is a potent and selective inhibitor of insulin-degrading enzyme (IDE) and NLRP3, with an IC50 of 188 nM against IDE. ML345 targets the Cys819 residue of IDE to inhibit IDE. ML345 selectively binds to NLRP3 in a non-covalent manner. ML345 inhibits inflammatory cytokines (IL-1β, IL-6) and exhibits potent anti-inflammatory activity. ML345 exerts a protective effect against miscarriage.
    ML345
  • HY-N0696
    Sipeimine
    		Inhibitor 98.57%
    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-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-N1431
    Tabersonine
    		Inhibitor 98.13%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
NOD-like Receptor (NLR) Isoform Comparison

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