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-161297A
    NT-0249 free base
    Inhibitor
    NT-0249 free base is an orally active NLRP3 inhibitor. NT-0249 has anti-inflammatory activity.
    NT-0249 free base
  • HY-P5524A
    C12-iE-DAP hydrochloride
    Agonist
    C12-iE-DAP hydrochloride is the hydrochloride salt form of C12-iE-DAP (HY-P5524). C12-iE-DAP hydrochloride is a biologically active peptide that has agonistic effects on NOD1.
    C12-iE-DAP hydrochloride
  • HY-156647
    Usnoflast
    Modulator 98.59%
    Usnoflast is the selective, orally active inhibitor for NLRP3 that blocks the release of IL-1β, and exhibits anti-inflammatory activity.
    Usnoflast
  • HY-163358
    SLC3037
    Inhibitor 99.85%
    SLC3037 is a NLRP3 inhibitor which blocks NLRP3 from binding to NEK7 or oligomerization, inhibiting inflammasome caused by MSU and other inflammasome activators. SLC3037 can be used for research of gout, cardiovascular diseases, metabolic syndrome or neurodegenerative diseases.
    SLC3037
  • HY-143563
    NLRP3 antagonist 1
    Antagonist 98.86%
    NLRP3 antagonist 1 is a potent antagonist of NLRP3. NLRP3 is mainly expressed in macrophages and neutrophils and is involved in the body's intrinsic immunity against pathogenic infections and stress injury. NLRP3 antagonist 1 has the potential for the research of cancer disease (extracted from patent WO2021114691A1, compound 3).
    NLRP3 antagonist 1
  • HY-147506
    NOD2 antagonist 1
    Antagonist 99.57%
    NOD2 antagonist 1 (compound 32) is a potent and selective NOD2 antagonist with an IC50 of 5.23 μM. NOD2 antagonist 1 inhibits Muramyl dipeptide (MDP)-induced IL-8 secretion in THP-1 cells and inhibits MDP-induced IL-6, IL-10, TNF-α release in PBMCs.
    NOD2 antagonist 1
  • HY-176860
    NEK7 degrader-1
    Activator 99.94%
    NEK7 degrader-1 is a NEK7 molecular glue degrader with a DC50 of 9  nM. NEK7 degrader-1 dose-dependently inhibits caspase-1 activity and IL-Ιβ release in macrophages in response to NLRP3 inflammasome activation. NEK7 degrader-1 can be used for autoinflammatory and autoimmune disorders like multiple sclerosis, neurodegeneraive diseases like Alzheimer's disease and cardiovascular and melabolic disorders like pericarditis and Type 2 diabetes research.
    NEK7 degrader-1
  • HY-17355B
    Dexpramipexole
    Inhibitor 99.56%
    Dexpramipexole ((R)-Pramipexole) is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Nav1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole induces mitophagy, inhibits ferroptosis, pyroptosis, apoptosis, neuroinflammation and eosinophilopoiesis; maintains mitochondrial function and redox homeostasis; reduces reactive oxygen species production; and decreases myocardial infarct size. Dexpramipexole is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more.
    Dexpramipexole
  • HY-130252
    YQ128
    Inhibitor 99.74%
    YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 μM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity. YQ128 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    YQ128
  • HY-163159
    NP3-562
    Inhibitor 98.16%
    NP3-562 is an orally active NLRP3 Inhibitor. NP3-562 inhibits IL-1β release in the supernatant of Nigericin (HY-127019)-stimulated THP-1 cells (IC50 = 66 nM), human whole blood (IC50 = 214 nM) and a mouse acute peritonitis model. NP3-562 can be used for the study of acute peritonitis.
    NP3-562
  • HY-P5523A
    iE-DAP dihydrochloride
    Agonist 99.72%
    iE-DAP dihydrochloride is a Nod1 agonist. iE-DAP dihydrochloride activates NOD1, which in turn activates the NF-κB signaling pathway and MLCK signaling pathway, inducing cellular inflammatory responses and tight junction disruption. iE-DAP dihydrochloride downregulates the expression of ZO-1 and Occludin genes. iE-DAP dihydrochloride increases the secretion of IL-6, GRO-α, MCP-1, IL-8 and MIP-1β in term human trophoblast cell cultures. iE-DAP dihydrochloride triggers preterm birth in pregnant mice, reduces fetal body weight, and induces fetal inflammation. iE-DAP dihydrochloride can be used in studies related to mastitis and preterm birth.
    iE-DAP dihydrochloride
  • HY-137245
    Emlenoflast
    Inhibitor 99.30%
    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-137553
    β-Aminoarteether
    Inhibitor 99.29%
    β-Aminoarteether (SM934 free base) is an Artemisinin derivative with orally active. β-Aminoarteether can be used for inflammation and autoimmune disease research, such as lupus diseases.
    β-Aminoarteether
  • HY-13682B
    Mifamurtide sodium
    98.19%
    Mifamurtide sodium (MTP-PE sodium), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide sodium is a specific ligand for NOD2 and acts as an insulin sensitizer. Mifamurtide sodium has potential for use in rare disease and osteosarcoma research.
    Mifamurtide sodium
  • HY-119721
    CP-424174
    Inhibitor 98.69%
    CP-424174 is a reversible inhibitor against IL-1β processing with an IC50 of 210 nM.CP-424174 indirectly inhibits NLRP3.
    CP-424174
  • HY-N2157
    Pteryxin
    Inhibitor 99.55%
    Pteryxin ((+)-Pteryxin) is an orally active multi-target inhibitor that targets NF-κB, MAPK, NLRP3 inflammasome, and Nrf2/ARE pathways. Pteryxin is also a BChE inhibitor (IC50=12.96 μg/mL) with a low inhibitory efficiency on AChE. Pteryxin inhibits the Ca2+-calcineurin-NFATc1 pathway by blocking NF-κB/MAPK signaling, inhibiting NLRP3 inflammasome activation, and reducing ROS generation, and activates Nrf2-mediated antioxidant enzyme expression. Pteryxin has anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin can be used in the study of inflammatory diseases, osteoporosis, diabetes, and Alzheimer's disease.
    Pteryxin
  • HY-151252
    NIC-0102
    Inhibitor 98.72%
    NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β.
    NIC-0102
  • HY-155751
    HMGB1-IN-1
    Inhibitor 98.40%
    HMGB1-IN-1 (compound 6) displays strong NO inhibitory effect in RAW264.7 cells with IC50 value of 15.9 ± 0.6 μM. HMGB1-IN-1 inhibit the HMGB1/NF-κB/NLRP3 pathway. HMGB1-IN-1 shows good anti-inflammatory activity and good anti-sepsis effects in kidney injury.
    HMGB1-IN-1
  • HY-N0921
    Dihydromethysticin
    Activator 99.71%
    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-W923189
    Neral
    Inhibitor
    Neral is a plant-derived anti-inflammatory, antioxidant and anticancer agent. Neral inhibits the phosphorylation of ERK1/2, p38 MAPK and IκB in macrophages induced by LPS (HY-D1056), suppresses the secretion of TNF-α and IL-6, as well as the expression of pro-IL-1β, iNOS and COX-2 in cells, and reduces the production of ROS in cells. Neral inhibits the activation of the NLRP3 inflammasome, and decreases the activation of caspase-1 and the secretion of IL-1β in mouse macrophages. Neral induces autophagy, and exhibits antiproliferative activity both in in vitro breast cancer cell models and mouse xenograft models. Neral regulates brassinosteroid, jasmonic acid and ethylene signaling pathways, and induces the expression of AP2/ERF-ERF and bHLH family genes in rice roots. Neral acts as a herbicide safener, alleviates the damage induced by Fenoxaprop-P-ethyl (HY-B2013), and promotes the elongation of rice roots. Neral can be used in research related to breast cancer, inflammatory and immune system diseases, and herbicide safeners.
    Neral
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