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

NOD-like Receptor (NLR)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B0516AR
    Articaine (Standard)
    Inhibitor
    Articaine (Standard) is the analytical standard of Articaine (HY-B0516A). This product is intended for research and analytical applications. Articaine (Hoe-045) hydrochloride is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC50 of 15.8 μM for open-state Na+ channels, and IC50 of 40.6 μM and 378 μM for inactivated and resting-state Na+ channels, respectively. Articaine hydrochloride exerts local anesthetic activity by inhibiting Na+ influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine hydrochloride can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury).
    Articaine (Standard)
  • HY-159898
    AChE/BChE-IN-23
    Inhibitor
    AChE/BChE-IN-23 (Compound 6e) is an AChE/BChE inhibitor (IC50: 0.91 μM, 1.19 μM and 1.01 μM for hAChE, eq BChE and hBChE, respectively). AChE/BChE-IN-23 has antioxidant activity and inhibits 1-42 and Tau protein aggregation. AChE/BChE-IN-23 also inhibits microglial activation by reducing ROS release and mitochondrial injury. AChE/BChE-IN-23 suppresses NLRP3 inflammasome and pro-inflammatory cytokines in human microglial cells. AChE/BChE-IN-23 also reverses the Scopolamine (HY-N0296)-induced memory impairment in mice model.
    AChE/BChE-IN-23
  • HY-168594
    α-Glucosidase/NLRP3-IN-1
    Inhibitor
    α-Glucosidase/NLRP3-IN-1 (Compound 8) is a dual inhibitor of α-glucosidase and NLRP3, exhibiting an IC50 of 6.6 μM against α-glucosidase and inhibiting NLRP3 in multiple cell lines at a concentration of 100 μM. α-Glucosidase/NLRP3-IN-1 demonstrates neuroprotective and antidiabetic properties, and can be utilized in relevant research.
    α-Glucosidase/NLRP3-IN-1
  • HY-161120
    NLRP3-IN-27
    Inhibitor
    NLRP3-IN-27 is a selective NLRP3 inhibitor with a IC50 value of 0.55 μM. NLRP3-IN-27 can be used in the study of inflammation and immunity.
    NLRP3-IN-27
  • HY-132591C
    Inclisiran sodium scrambled negative control
    Inhibitor
    Inclisiran sodium scrambled negative control is the sequence scrambled negative control of Inclisiran sodium.
    Inclisiran sodium scrambled negative control
  • HY-P5522
    TriDAP
    Activator
    TriDAP (L-Ala-γ-D-Glu-meso-diaminopimelic acid) is a NOD1 agonist with a Kd value of 34.5 μM. TriDAP enhances the binding of NOD1-RICK, promotes RICK phosphorylation, and activates the NF-κB, TAK1, MEK/ERK, p38 and interferon response pathways. TriDAP downregulates Runx2 via increasing ubiquitination and reduces trabecular bone parameters. TriDAP decreases IκBα levels and increases p65 levels. TriDAP 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 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 can be used in research related to pulpitis, chronic ulcerative colitis, Crohn's disease and SARS-CoV-2 infection.
    TriDAP
  • HY-170950
    P2Y14 antagonist 1
    Inhibitor
    P2Y14 antagonist 1 (compound 45) is a high selective and orally active P2Y14R antagonist with an IC50 of 0.70 nM. P2Y14R antagonist 1 demonstrates significant anti-inflammatory efficacy, effectively mitigating the pulmonary infiltration of immune cells and inflammatory response through suppressing the NLRP3 signaling pathway. P2Y14R antagonist 1 has the potential for the research of acute lung injury.
    P2Y14 antagonist 1
  • HY-N0373R
    Licochalcone B (Standard)
    Inhibitor
    Licochalcone B (Standard) is the analytical standard of Licochalcone B. This product is intended for research and analytical applications. Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction.
    Licochalcone B (Standard)
  • HY-180830
    NLRP3-IN-86
    Inhibitor
    NLRP3-IN-86 (Compound 8a), a derivative of Songorine (HY-N2080), is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-86 can reduce LPS (HY-D1056)- and Nigericin (HY-127019)-stimulated lactate dehydrogenase (LDH) release (IC50 = 2.69 μM in THP-1 cells and 1.75 μ M in J774A.1 cells). NLRP3-IN-86 can inhibit gasdermin D (GSDMD) cleavage and IL-1β secretion. NLRP3-IN-86 can inhibit cell pyroptosis. NLRP3-IN-86 can be used for research of inflammation.
    NLRP3-IN-86
  • HY-145911
    NLRP3-IN-7
    Inhibitor
    NLRP3-IN-7 (Compound 36) is a selective NLRP3 inflammasome inhibitor. NLRP3-IN-7 effectively blocks the assembly of the NLRP3 inflammasome.
    NLRP3-IN-7
  • HY-168158
    NOD2 agonist 3
    Agonist
    NOD2 agonist 3 (Compound 5) is a potent NOD2 agonist, with an EC50 of 111.45 nM. NOD2 agonist 3 shows immunopotentiating effects.
    NOD2 agonist 3
  • HY-179009
    NOD2 agonist 4
    Agonist
    NOD2 agonist 4 (Compound 12b) is a potent NOD2 agonist with an EC50 of 44.1 nM. NOD2 agonist 4 induces cytokine production (MCP-1, IL-6 and IL-8) in peripheral blood mononuclear cells (PBMCs), both alone and in combination with Lipopolysaccharide (LPS) (HY-D1056). NOD2 agonist 4 can be used for the studies of NOD2-targeted immunomodulator or vaccine adjuvant.
    NOD2 agonist 4
  • HY-P11581
    MNP2
    Inhibitor
    MNP2 is a NLRP3-ASC interaction inhibitor. MNP2 selectively binds to the PYD domain of ASC (Ka=149 nM) and blocks ASC-PYM binding (Ka=58 nM), thereby inhibiting the interaction between ASC and NLRP3 and suppressing the formation of the NLRP3 inflammasome. MNP2 inhibits IL-1β release and caspase-1 maturation, and reduces the efflux of potassium and chloride ions. MNP2 prevents mitochondrial damage and reactive oxygen species production, and significantly decreases NLRP3 inflammasome formation in neurodegenerative pathologies induced by β-amyloid, Tau protein and α-synuclein. MNP2 is applicable for the research of neurodegenerative diseases.
    MNP2
  • HY-182803
    NLRP3-IN-90
    Inhibitor
    NLRP3-IN-90 (Compound 1) is a NLRP3 inflammasome inhibitor. NLRP3-IN-90 is applicable for inflammation research.
    NLRP3-IN-90
  • HY-146594
    NLRP3-IN-8
    Inhibitor
    NLRP3-IN-8 (compound 27) is an orally active, directly binding NLRP3 inflammasome inhibitor with an IC50 value of 1.23 μM against IL-1 β. NLRP3-IN-8 has good metabolic stability to liver microsomes (t1/2 = 138.63 min), and has almost no toxicity (against L02: IC50 > 100 μM).
    NLRP3-IN-8
  • HY-160545
    NLRP3-IN-31
    Inhibitor
    NLRP3-IN-31 (Comp 14) is a NLRP3 inhibitor, with an IC50 of 0.3-0.5 μM.
    NLRP3-IN-31
  • HY-149122
    NLRP3-IN-15
    Inhibitor
    NLRP3-IN-15 is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-15 inhibits IL-1β release with an IC50 of 0.114 μM. NLRP3-IN-15 can be used for the research of inflammation.
    NLRP3-IN-15
  • HY-148258A
    GDC-2394 sodium
    Inhibitor
    GDC-2394 (Compound 20) sodium 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 sodium inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation. GDC-2394 sodium could be used to study gouty arthritis.
    GDC-2394 sodium
  • HY-157146
    NLRP3-IN-23
    Inhibitor
    NLRP3-IN-23 (Compound 15C) is an inhibitor of heme-mediated induction of the NLRP3 inflammasome. NLRP3-IN-23 significantly inhibits heme-mediated induction of the NLRP3 inflammasome at a concentration of 0.1 μM.
    NLRP3-IN-23
  • HY-178953
    NLRP3-IN-84
    Inhibitor
    NLRP3-IN-84 (Compound 32) is a NLRP3 inflammasome inhibitor. NLRP3-IN-84 can interfere with the oligomerization process of NLRP3 by inhibiting the activity of NLRP3 ATPase (IC50 = 158.4 nM). NLRP3-IN-84 inhibits Caspase-1 (IC50 = 27.7 nM), IL-1β release (PBMC: IC50 = 19.5 nM; mPBMC: IC50 = 24.2 nM), and ASC plaque formation (IC50 = 131 nM). NLRP3-IN-84 has no inhibitory activity on NLRC4 and AIM2 inflammasomes. NLRP3-IN-84 exhibits significant in vivo anti-inflammatory effects in a mouse acute peritonitis model. NLRP3-IN-84 can be used for the study of NLRP3-related inflammatory diseases.
    NLRP3-IN-84
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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