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-170904
    NLRP3-IN-72
    		Inhibitor
    NLRP3-IN-72 (Compound 2) is a benzimidazole derivative. NLRP3-IN-72 exhibits anti-inflammatory and antioxidant activities. NLRP3-IN-72 has an IC50 of 0.3 μM for NLRP3 IL-1β, a PD50 of 0.4 μM for protecting against pyroptosis, and an EC50 of 0.6 μM for inducing HO-1.
    NLRP3-IN-72
  • HY-163744
    NLRP3-IN-42
    		Inhibitor
    NLRP3-IN-42 (compound H28) is a potent NLRP3 inhibitor with an KD value of 1.15 µM. NLRP3-IN-42 decreases the LPS (HY-D1056) induced protein expression of cleaved-caspase-1 (p20). NLRP3-IN-42 selectively inhibits IL-1β release.
    NLRP3-IN-42
  • HY-162846
    NLRP3-IN-44
    		Inhibitor
    NLRP3-IN-44 (compound P33) is a potent and orally active (approximately 62%) inhibitor of NLRP3, with the Kd of 17.5 nM. NLRP3-IN-44 plays an important for studying NLRP3 inflammasome-mediated diseases.
    NLRP3-IN-44
  • HY-175814
    NLRP3-IN-83
    		Inhibitor
    NLRP3-IN-83 is a selective and orally active NLRP3 inflammasome activation inhibitor. NLRP3-IN-83 exhibits good inhibitory IL-1β activity with an IC50 of 1.4 μM by blocking NLRP3, independent of NF-κB signaling. NLRP3-IN-83 only slightly inhibits AIM2 inflammasome pathway, but has no effect on NLRC4 inflammasome. NLRP3-IN-83 prevent cell pyroptosis and exhibits significant anti-inflammatory efficacy in ulcerative colitis model. NLRP3-IN-83 can be used for the study of inflammatory bowel disease (IBD).
    NLRP3-IN-83
  • HY-168137
    NOD2 agonist 2
    		Agonist
    NOD2 agonist 2 (compound 23) enhanced the antigen presentation of mouse bone marrow-derived dendritic cells (BMDCs), highlighting its potential as a vaccine adjuvant.
    NOD2 agonist 2
  • HY-137553A
    β-Aminoarteether maleate
    		Inhibitor
    β-Aminoarteether maleate (SM934) is an Artemisinin derivative with orally active. β-Aminoarteether maleate can be used for inflammation and autoimmune disease research, such as lupus diseases.
    β-Aminoarteether maleate
  • HY-178898
    7-Oxogedunin
    		Inhibitor
    7-Oxogedunin (Compound 7DG; Compound 16) is a small molecule that protects macrophages from cell pyroptosis induced by anthrax lethal toxin (LT). Its target is protein kinase R (PKR). 7-Oxogedunin can widely inhibit the assembly of various inflammasomes (NLRP1 and NLRP3) and the activation of caspase-1 by inhibiting the kinase-independent function of PKR. 7-Oxogedunin has growth inhibitory activity on European corn borer larvae. 7-Oxogedunin can be used for LT toxicity inhibition and pest control research.
    7-Oxogedunin
  • HY-N0496R
    Ruscogenin (Standard)
    		Inhibitor
    Ruscogenin (Standard) is the analytical standard of Ruscogenin. This product is intended for research and analytical applications. Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway. Ruscogenin exerts significant anti-inflammatory and anti-thrombotic activities. Ruscogenin has orally bioactivity.
    Ruscogenin (Standard)
  • HY-182287
    PRDX1-IN-4
    		Inhibitor
    PRDX1-IN-4 is a PRDX1 inhibitor with an IC50 of 122 nM against human targets and high subtype selectivity. PRDX1-IN-4 covalently binds to PRDX1 to promote ROS accumulation. PRDX1-IN-4 inhibits NLRP3 inflammasome activation, blocks hepatic stellate cell activation and reduces collagen deposition. PRDX1-IN-4 induces apoptosis in activated hepatic stellate cells. PRDX1-IN-4 has good safety profile, with no significant body weight loss or hepatotoxicity observed in mice at a dose of 20 mg/kg. PRDX1-IN-4 ameliorates CCl4-induced liver injury and liver fibrosis in mice at a dose of 1 mg/kg. PRDX1-IN-4 can be used for the research of liver fibrosis.
    PRDX1-IN-4
  • HY-168503
    NLRP3-IN-54
    		Inhibitor
    NLRP3-IN-54 (Compound C4) is an NLRP3 inhibitor. NLRP3-IN-54 can significantly reduce the levels of active Caspase-1 and active IL-1β (IC50 = 0.805 μM), can be used for inflammation research.
    NLRP3-IN-54
  • HY-172134
    NLRP3-IN-70
    		Inhibitor
    NLRP3-IN-70 (Compound 5m) is an NLRP3 inflammasome inhibitor with low oral bioavailability. NLRP3-IN-70 can directly bind to the NACHT domain of the NLRP3 protein and block the interaction of NLRP3 and ASC, thus inhibiting ASC oligomerization and NLRP3 inflammasome assembly. NLRP3-IN-70 can be used in the research of sepsis and nonalcoholic steatohepatitis.
    NLRP3-IN-70
  • HY-157555
    NLRP3-IN-29
    		Inhibitor
    NLRP3-IN-29(Compound 5M) is an inhibitor of NLR family pyrin domain containing 3 (NLRP3). NLRP3-IN-29 has the potential for blood-brain barrier permeability and inflammation inhibition both in vivo and in vitro. NLRP3-IN-29 can be used for research on Alzheimer's disease.
    NLRP3-IN-29
  • HY-181809
    BLT1-IN-1
    		Inhibitor
    BLT1-IN-1 is an orally active and selective BLT1 inhibitor with an IC50 of 8.7 nM and a Kd of 121 nM. BLT1-IN-1 exerts protective effects against acute lung injury and sepsis in in vivo models. BLT1-IN-1 can be used in research related to acute lung injury and sepsis.
    BLT1-IN-1
  • HY-183796
    GFAP/NF-κB/APOE/NLRP3-IN-1
    		Inhibitor
    GFAP/NF-κB/APOE/NLRP3-IN-1 (Compound 11a) is an orally active, blood-brain barrier-permeable multi-target inhibitor with an IC50 of 3.50 nM against Acetylcholinesterase. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits BACE-1 with an IC50 of 14.61 nM. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits Aβ1-42 aggregation with an IC50 of 8.63 μM. GFAP/NF-κB/APOE/NLRP3-IN-1 reduces the levels of GFAP, NLRP3 inflammasome, NF-κB and APOE. GFAP/NF-κB/APOE/NLRP3-IN-1 is applicable for the research of Alzheimer's disease and neuroblastoma.
    GFAP/NF-κB/APOE/NLRP3-IN-1
  • HY-N10312
    Yadanzigan
    		Inhibitor
    Yadanzigan (YDZG) is an anti-inflammatory agent and a NLRP3 inhibitor. Yadanzigan specifically inhibits NLRP3 activation via inhibiting NF-κB pathway and Reactive Oxygen Species production. Yadanzigan also moderates LPS (HY-D1056)-induced acute lung injury (ALI) in mice.
    Yadanzigan
  • HY-185311
    NEK7 degrader-3
    		Inhibitor
    NEK7 degrader-3 is an orally active and brain-penetrant NEK7 molecular glue degrader with a DC50 of 33.1 nM. NEK7 degrader-3 mediates interaction between NEK7 and E3 ligase cereblon, promoting proteasomal degradation of NEK7 and attenuating NLRP3 inflammasome-mediated inflammatory responses. NEK7 degrader-3 inhibits caspase-1 activity, cytokine release of IL-1β, IL-1α, and IL-18, and pyroptosis-related plasma membrane permeabilization. NEK7 degrader-3 shows antiinflammatory activity in an LPS (HY-D1056)-induced neuroinflammation mouse model. NEK7 degrader-3 can be used for the research of neuroinflammation.
    NEK7 degrader-3
  • HY-146802
    NLRP3-IN-9
    		Inhibitor
    NLRP3-IN-9 is a potent NLRP3 inhibitor. NLRP3-IN-9 inhibits IL-1β release. NLRP3-IN-9 reduces inflammation and mechanical hyperalgesia. NLRP3-IN-9 has the potential for the research of gout.
    NLRP3-IN-9
  • HY-163756
    NLRP3-IN-43
    		Inhibitor
    NLRP3-IN-43 (compound II-8) is a poteny inhibitor of NLRP3 inflammasome activation that binds to the LRR domain, and disrupts NLRP3-NEK7 interaction.
    NLRP3-IN-43
  • HY-179387
    CXCR2-IN-3
    		Inhibitor
    CXCR2-IN-3 is a CXCR2 inhibitor with an IC50 of 11.37 μM. CXCR2-IN-3 mediates CXCR2-Ca2+ signalling inhibition halted autophagic flux, subsequently facilitating ROS-mediated apoptotic cell death. CXCR2-IN-3 suppresses the CXCR2-NLRP3 canonical pathway, suppressing pre-tumorigenic markers. CXCR2-IN-3 causes autophagy-dependent cell death in polyploid giant cancer cells (PGCCs). CXCR2-IN-3 can be used for the research of oral squamous cell carcinoma (OSCC).
    CXCR2-IN-3
  • HY-17355AR
    Dexpramipexole dihydrochloride (Standard)
    		Inhibitor
    Dexpramipexole ((R)-Pramipexole) dihydrochloride (Standard) is the analytical standard of Dexpramipexole (dihydrochloride). This product is intended for research and analytical applications. Dexpramipexole dihydrochloride is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole dihydrochloride 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 dihydrochloride 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 dihydrochloride is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more.
    Dexpramipexole dihydrochloride (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
NOD-like Receptor (NLR) Isoform Comparison

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