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-157554
    ZM640
    		Inhibitor
    ZM640 is a NLRP3 inhibitor. ZM640 enhances IL-1β release mediated by NLRP3 inflammasome activation in THP-1 cells. ZM640 shows low cytotoxicity.
    ZM640
  • HY-103715
    NLRP3 modulator 1
    		Modulator
    NLRP3 modulator 1 is the potent modulator of NLRP3. NLRP3 modulator 1 agonizes or partially agonizes NLRP3 that are useful for researching a condition, disease or disorder in which a decrease in LRP3 activity contributes to the pathology (extracted from patent WO2017184746A1, compound 107).
    NLRP3 modulator 1
  • HY-179503
    PDE/TRPA1/CHIT1-IN-1
    		Inhibitor
    PDE/TRPA1/CHIT1-IN-1 is a phosphodiesterases (PDEs), TRPA1, and hCHIT1 (KD of 37.7 μM) inhibitor. PDE/TRPA1/CHIT1-IN-1 is a broad-spectrum PDE inhibitor, potently targeting key isoforms including PDE4B, PDE7A, PDE3A, and PDE8A with IC50s of 15.54, 15.15, 8.39 and 16.46 μM. PDE/TRPA1/CHIT1-IN-1 suppresses NLRP3 inflammasome activation and inhibits NF-κB phosphorylation, downregulating the expression of pro-inflammatory genes (TNF-α and IL-6) in vivo. PDE/TRPA1/CHIT1-IN-1 can be used for chronic obstructive pulmonary disease (COPD) and related inflammatory lung disorders research.
    PDE/TRPA1/CHIT1-IN-1
  • HY-170529
    NLRP3-IN-61
    		Inhibitor
    NLRP3-IN-61 (Compound 1) is an inhibitor for NLRP3. NLRP3-IN-61 inhibits pyroptosis in THP-1 cell with an IC50 of 12.6 nM, inhibits IL-β release with an IC50 of 25.3 nM.
    NLRP3-IN-61
  • HY-N19847
    LYRM03
    		Inhibitor
    LYRM03 is a derivative of Ubenimex (HY-B0134) and a Aminopeptidase N inhibitor. LYRM03 is isolated from Streptomyces HCCB10043. LYRM03 inhibits TLR4, MyD88, NLRP3, ASC, NF-κB and p38 MAPK, stabilizes IκB, and suppresses LPS-induced expression of iNOS and COX-2. LYRM03 reduces the levels of inflammatory cytokines and oxidative stress markers, and alleviates pulmonary edema. LYRM03 exhibits anticancer activity against breast cancer. LYRM03 has anti-inflammatory activity. LYRM03 can be used in the research of acute lung injury and breast cancer.
    LYRM03
  • HY-163274
    NOD1 antagonist-1
    		Antagonist
    NOD1 antagonist-1 (compound 37) exhibits an antagonistic activity towards NOD1 and a weak NOD1/NOD2 selectivity, with IC50s of 9.18 μM and 20.8 μM, respectively.
    NOD1 antagonist-1
  • HY-159718
    NLRP3-IN-46
    		Inhibitor
    NLRP3-IN-46 (Compound 3k) activates neuro-immunomodulatory cholinergic anti-inflammatory pathway, and thus inhibits NLRP3 inflammasome activation. NLRP3-IN-46 inhibits Uric acid sodium (HY-B2130A)-induced IL-1β production in THP-1 cells, and can be used in gouty arthritis research.
    NLRP3-IN-46
  • HY-159965
    NOD1-RIPK2-IN-1
    		Inhibitor
    NOD1-RIPK2-IN-1 (Compound 37) is a NOD1-RIPK2 signaling pathway inhibitor with IC50 values of 42 nM and 1.52 nM for NOD1 and RIPK2, respectively. NOD1-RIPK2-IN-1 reduces the secretion of the pro-inflammatory cytokine IL-8 and can be used in the research of inflammation and immune-related diseases.
    NOD1-RIPK2-IN-1
  • HY-175645
    NLRP3/URAT1-IN-1
    		Inhibitor
    NLRP3/URAT1-IN-1 is an orally active double inhibitor of NLRP3 and URAT1 (IC50 = 3.81 μM). NLRP3/URAT1-IN-1 inhibits IL-1β release in LPS (HY-D1056) and ATP-stimulated mouse bone marrow-derived macrophages (BMDMs), with an IC50 of 2.61 μM. NLRP3/URAT1-IN-1 reduces serum uric acid (SUA) and alleviates liver/kidney damage in mice with acute hyperuricemia (HUA). NLRP3/URAT1-IN-1can be used for the study of gout and hyperuricemia.
    NLRP3/URAT1-IN-1
  • HY-113298R
    Citraconic acid (Standard)
    		Inhibitor
    Citraconic acid (Methylmaleic acid) (Standard) is the analytical standard of Citraconic acid (HY-113298). This product is intended for research and analytical applications. Citraconic acid is an orally active inhibitor targeting the NLRP3 inflammasome and Keap1-Nrf2 pathway. Citraconic acid reduces reactive oxygen species (ROS) generation by inhibiting succinate dehydrogenase (SDH) activity. Citraconic acid also modifies the conformation of Keap1 protein, relieves its inhibition of Nrf2, promotes antioxidant gene expression, and inhibits NLRP3 activation and the release of pro-inflammatory factors such as IL-1β and IL-18. Citraconic acid has anti-inflammatory and antioxidant activities, can reduce oxidative stress and cell pyroptosis, improve tissue damage, and can be used for the research of inflammation-related diseases such as acute renal ischemia-reperfusion injury. Citraconic acid is an isomer of Itaconic acid (HY-Y052).
    Citraconic acid (Standard)
  • HY-182380
    ODZ10117
    		Inhibitor
    ODZ10117 is a STAT3 and NLRP3 inhibitor with a human STAT3 SH2 domain IC50 of 7.5 μM. ODZ10117 binds to the STAT3 SH2 domain, suppressing tyrosine phosphorylation, dimerization, nuclear translocation, and transcriptional activity. ODZ10117 binds to NLRP3, impairs NEK7 interaction, prevents inflammasome formation, and inhibits caspase-1 and IL-1β cleavage.ODZ10117 reduces MSU (HY-B2130A)-induced IL-1β release, lowers LPS (HY-D1056)-induced sepsis mortality, and exhibits anti-inflammatory effects. ODZ10117 induces apoptosis, suppresses breast cancer cell migration and invasion, reduces tumor growth and lung metastasis, and extends survival in breast cancer models. ODZ10117 can be used for the research of Monosodium urate (HY-B2130A)-induced peritonitis, LPS-induced sepsis, breast cancer, glioblastoma, and Alzheimer's disease.
    ODZ10117
  • HY-178950
    Hck-IN-3
    		Inhibitor
    Hck-IN-3 (compound 2D) is an orally effective inhibitor targeting HCK (KD = 3.92 μM). Hck-IN-3 can inhibit the release of NO. Hck-IN-3 has an IC50 of 6.52 μM in RAW264.7 cells. Hck-IN-3 can inhibit the release of TNF-α, IL-6, and IL-1β in a concentration dependent manner. Hck-IN-3 downregulates the protein expression of NLRP3, ASC, pro-caspase-1, and pro-IL-1β in a concentration dependent manner. Hck-IN-3 can be used for research on acute non traumatic inflammatory conditions.
    Hck-IN-3
  • HY-14644B
    Apilimod hydrochloride
    		Inhibitor
    Apilimod (STA 5326) hydrochloride is a PIKFYVE kinase inhibitor that promotes NLRP3 inflammatory vesicle activation and IL-1β secretion. Apilimod hydrochloride has been shown to inhibit host cell proteases, which may prevent viral invasion but also block antiviral immune responses, potentially exacerbating immunosuppression in COVID-19.
    Apilimod hydrochloride
  • HY-173294
    NLRP3-IN-74
    		Inhibitor
    NLRP3-IN-74 (Compound 11) is an orally active NLRP3 inhibitor with an IC50 value of 2.7 μM. NLRP3-IN-74 can inhibit the release of IL-1β, reducing the release level by approximately 90%, and does not inhibit the release of TNFα. NLRP3-IN-74 can be used in the research of related diseases such as atherosclerosis and Parkinson's disease.
    NLRP3-IN-74
  • HY-163493
    NLRP3-IN-35
    		Inhibitor
    NLRP3-IN-35 (compound 11) is an NLRP3 inhibitor (IC50 < 1 μM).
    NLRP3-IN-35
  • HY-B0516R
    Articaine hydrochloride (Standard)
    		Inhibitor
    Articaine (Hoe-045) hydrochloride (Standard) is the analytical standard of Articaine hydrochloride (HY-B0516). 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 hydrochloride (Standard)
  • HY-168159
    TLR7 agonist 27
    		Agonist
    TLR7 agonist 27 (compound 24) is a potent TLR7 agonist with an EC50 of 238.1 nM. TLR7 agonist 27 shows weak agonistic activity against NOD2 (nucleotide-binding oligomerization domain 2) (EC50 of 6.2 μM). TLR7 agonist 27 is a potent immunostimulant, and can be used as a vaccine adjuvant and/or immunotherapeutic.
    TLR7 agonist 27
  • HY-170447
    NOD1 antagonist-2
    		Antagonist
    NOD1 antagonist-2 (compound 66) is an orally active selective antagonist of both human and mouse NOD1. NOD1 antagonist-2 (compound 66) antagonizes NOD1-induced NF-κB and MAPK pathways.
    NOD1 antagonist-2
  • HY-168091
    YM-I-26
    		Inhibitor
    YM-I-26 is a selective NLRP3 inflammasome inhibitor. YM-I-26 enhances the phagocytosis of β-amyloid protein by mouse microglial BV2 cells and inhibits the production of IL-1β and IL-10. YM-I-26 can be used to study the immunomodulatory activity associated with inflammation.
    YM-I-26
  • HY-179429
    NLRP3-IN-85
    		Inhibitor
    NLRP3-IN-85 (compound 5d) is a potent NLRP3 inhibitor that targets mitochondria in a ΔΨm-independent manner. NLRP3-IN-85 protects mitochondria from oxidative stress and inflammation damage and suppresses key inflammatory factors (NO, TNF-α, IL-6). NLRP3-IN-85 relives acute lung injury in mice and inhibits paw edema in rats. NLRP3-IN-85 can be used for acute lung injury (ALI) research.
    NLRP3-IN-85
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
NOD-like Receptor (NLR) Isoform Comparison

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