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-132831C
    Selnoflast monopotassium
    		Inhibitor
    Selnoflast (RO7486967) monopotassium, formerly somalix/RG6418/IZD334 monopotassium, is an orally active, potent, selective and reversible small molecule NLRP3 inflammasome inhibitor. Selnoflast monopotassium is a potent inhibitor of IL-1β release stimulated by NLRP3 activation in human Alzheimer's disease (AD) monocyte-derived macrophages. Selnoflast monopotassium is promising for research of AD and systemic inflammatory diseases, such as ulcerative colitis and chronic obstructive pulmonary disease.
    Selnoflast monopotassium
  • HY-179132
    TN-101
    		Inhibitor
    TN-101 is an orally active NLRP3 inhibitor (IC50 = 29.8 nM). TN-101 can be used for the study of obesity.
    TN-101
  • HY-RS09406
    NOD2 Human Pre-designed siRNA Set A
    		Inhibitor

    NOD2 Human Pre-designed siRNA Set A contains three designed siRNAs for NOD2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    NOD2 Human Pre-designed siRNA Set A
  • HY-161266
    COX-2/NLRP3-IN-1
    		Inhibitor
    COX-2/NLRP3-IN-1 (Compound 6k) is a COX-2/NLRP3 inhibitor with a IC50 of 1.53 μM for COX-2. COX-2/NLRP3-IN-1 exerts anti-inflammatory effects by inhibiting the NF-κB/NLRP3 signaling pathway.
    COX-2/NLRP3-IN-1
  • HY-149087
    MR2938
    		Inhibitor
    MR2938 is a potent AChE inhibitor, with an IC50 of 5.04 μM. MR2938 also suppresses NO production obviously (IC50 = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research.
    MR2938
  • HY-180916
    CAII-IN-11
    		Inhibitor
    CAII-IN-11 (Compound A1) is a dual-target compound that contains a hCA II inhibitor (IC₅₀ = 2 nM) portion and a NO donor portion. CAII-IN-11 also has inhibitory activity against hCA IX, hCA XII, and hCA I, with IC50 values of 6, 3, and 152 nM respectively. CAII-IN-11 significantly increases the intracellular cGMP level in human trabecular meshwork cells. CAII-IN-11 reduces the apoptosis of retinal ganglion cells by reducing oxidative stress (ROS levels), inhibiting astrocytes and the NLRP3 inflammasome activation. CAII-IN-11 has hypotensive activity in rabbit models and can be used for the study of glaucoma.
    CAII-IN-11
  • HY-182102
    NLRP3-IN-88
    		Inhibitor
    NLRP3-IN-88 (Compound 1) is an NLRP3 inhibitor. NLRP3-IN-88 inhibits IL-1β. NLRP3-IN-88 can be used in research on intestinal diseases and inflammatory diseases.
    NLRP3-IN-88
  • HY-146034
    NOD1/2 antagonist-1
    		Antagonist
    NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX).
    NOD1/2 antagonist-1
  • HY-163497
    NLRP3-IN-38
    		Inhibitor
    NLRP3-IN-38 (Compound 18) is an inhibitor for NOD-like receptor protein 3 (NLRP3), that inhibits NLRP3 inflammasome activation with an EC50 of 23 nM.
    NLRP3-IN-38
  • HY-175464
    NLRP3-IN-82
    		Inhibitor
    NLRP3-IN-82 (Compound 2b) is a NLRP3IC50< 5 nM). NLRP3-IN-82 can be used for neurological diseases like Alzheimer's disease, inflammatory diseases like inflammatory bowel disease and metabolic disorders like obesity research.
    NLRP3-IN-82
  • HY-149121
    NLRP3-IN-14
    		Inhibitor
    NLRP3-IN-14 is a potent and selective NLRP3 inflammasome inhibitor (KD: 5.87 μM). NLRP3-IN-14 inhibits IL-1β release with an IC50 of 0.131 μM. NLRP3-IN-14 can be used for the research of inflammation.
    NLRP3-IN-14
  • HY-161329
    NLRP3-IN-32
    		Inhibitor
    NLRP3-IN-32 (compound 7a), a 3, 4-dihydronaphthalene-1(2H)-one derivative, is a potential NLRP3 inflammatory vesicles inhibitor. NLRP3-IN-32 can block the assembly and activation of NLRP3 inflammasome by down-regulating the expression of NLPR3 and apoptosis-associated speck-like protein containing a CARD (ASC), and inhibiting the production of reactive oxygen species (ROS) and other inflammatory mediators. NLRP3-IN-32 inhibits the phosphorylation of IκBα and NF-κB/p65 and the nuclear translocation of p65, thereby inhibiting NF-κB signaling.
    NLRP3-IN-32
  • HY-101927
    NOD1/2 antagonist-2
    		Antagonist
    NOD1/2 antagonist-2 (Compound 26BH) is a dual NOD1/NOD2 antagonist (IC50s: 2.36 μM and 4.16 μM for NOD1 and NOD2, respectively). NOD1/2 antagonist-2 inhibits both NF-κB and MAPK inflammatory signaling, thereby sensitizing Paclitaxel (HY-B0015) to suppress Lewis lung carcinoma growth.
    NOD1/2 antagonist-2
  • HY-B1239A
    Drofenine
    Drofenine (Cycloadiphene; Hexahydroadiphenine) is an brain-penetrant antispasmodic agent. Drofenine is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine ameliorates diabetic peripheral neuropathy -like pathology. Drofenine can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm.
    Drofenine
  • HY-180890
    PPARγ agonist-21
    		Inhibitor
    PPARγ agonist-21 (Compound 9a) is a PPARγ agonist with an EC50 of 3.12 μM. PPARγ agonist-21 activates PPAR-γ to inhibit NF-κB and attenuate NLRP3 inflammasome assembly. PPARγ agonist-21 blocks NLRP3-ASC and NLRP3-NEK7 interaction. PPARγ agonist-21 attenuates the severity of gouty arthritis.
    PPARγ agonist-21
  • HY-158111
    NLRP3-IN-34
    		Inhibitor
    NLRP3-IN-34 (Compound T10) is an inhibitor for NLRP3 inflammasome. NLRP3-IN-34 inhibits ROS production, NLRP3 inflammasome-dependent IL-1β production (IC50 is 0.48 μM in cells J774A.1), and inhibits pyroptosis. NLRP3-IN-34 exhibits anti-inflammatory activity against DSS-induced peritonitis.
    NLRP3-IN-34
  • HY-W011082R
    NLRP3-IN-2 (Standard)
    		Inhibitor
    NLRP3-IN-2 (Standard) is the analytical standard of NLRP3-IN-2. This product is intended for research and analytical applications. NLRP3-IN-2, an intermediate substrate in the synthesis of glyburide, inhibits the formation of the NLRP3 inflammasome in cardiomyocytes and limits the infarct size following myocardial ischemia/reperfusion in the mouse, without affecting glucose metabolism.
    NLRP3-IN-2 (Standard)
  • HY-145087
    NP3-146
    		Inhibitor
    NP3-146 is a NLRP3 inflammasome inhibitor through locking the NACHT domain of NLRP3. NP3-146 shows potent inhibitory activity against IL-1β release with an IC50 value of 0.171 μM in LPS (HY-D1056)/Nigericin (HY-127019)-stimulated BMDM cells. NP3-146 regulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants. NP3-146 can be used for the research of inflammatory diseases.
    NP3-146
  • HY-162013
    NLRP3-IN-26
    		Inhibitor
    NLRP3-IN-26 (compound 15Z) is a NLRP3 inhibitor with the IC50 of 0.13 μM. NLRP3-IN-26 can be used for DSS-induced colitis model study.
    NLRP3-IN-26
  • HY-173046
    NLRP3-IN-71
    		Inhibitor
    NLRP3-IN-71 (Compound 19) is a BBB-permeable, orally active and selective NLRP3 inhibitor that can inhibit IL-1β secretion. NLRP3-IN-71 can be used for the research of neurodegenerative diseases.
    NLRP3-IN-71
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
NOD-like Receptor (NLR) Isoform Comparison

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