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-182779
    JNUTS013
    Inhibitor
    JNUTS013 is a NLRP3 inflammasome inhibitor. JNUTS013 promotes proteasome-dependent degradation of NLRP3 and inhibits the release of downstream cytokines. JNUTS013 downregulates the expression of inflammation-related proteins including iNOS and COX-2. JNUTS013 exhibits anti-inflammatory activity and can be used in the research of inflammatory diseases.
    JNUTS013
  • HY-172778
    HNW005
    Inhibitor
    HNW005 is a dual inhibitor of NLRP3 inflammasome and urate transporter 1 (URAT1). It has a KD value of 204.6 nM and an IC50 of 1.7 μM for inhibiting NLRP3 inflammasome activation, and an IC50 of 6.4 μM for inhibiting uric acid transmembrane transport. When administered at a dose of 2 mg/kg in vivo, HNW005 can achieve a uric acid reduction rate of 64.8%. It can exert anti - inflammatory, analgesic, and uric acid - lowering activities by inhibiting the activation of NLRP3 inflammasome and uric acid transmembrane transport. HNW005 can be used in the research of gouty arthritis.
    HNW005
  • HY-N17383
    Ligusticum cycloprolactam
    Inhibitor
    Ligusticum cycloprolactam is a potent, orally active, and CNS-penetrant TLR4/NF-κB inhibitor, exhibiting anti-inflammatory and neuroprotective activity. Ligusticum cycloprolactam reduces FPR1 expression, inhibits NLRP3 inflammasome, TLR4/NF-κB, hepatic MAPK and TGF-β signaling, and selectively activates hepatic FXR. Ligusticum cycloprolactam attenuates pro-inflammatory mediator production, enhances anti-inflammatory cytokine secretion, regulates renal uric acid transporters, and preserves intestinal microbiota composition. Ligusticum cycloprolactam can be used for the research of ischemic stroke, hyperuricemic nephropathy, neuroinflammation, and metabolic dysfunction-associated fatty liver disease.
    Ligusticum cycloprolactam
  • HY-163695
    NLRP3-IN-41
    Inhibitor
    NLRP3-IN-41 (compd S-9) is an orally active and brain-penetrant NLRP3 inhibitor with anti-inflammatory activities, anti-neuroinflammatory effect and without obvious cytotoxicity. NLRP3-IN-41 inhibits the priming and activation stages of the NLRP3 inflammasome and can be used for inflammasome-related diseases research.
    NLRP3-IN-41
  • HY-B2176S8
    ATP-13C10,15N5,d14 (dilithium)
    ATP-13C10,15N5,d14 (Adenosine 5'-triphosphate-13C10,15N5,d14) dilithium is the 13C-, 15N- and deuterium labeled ATP dilithium. ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation. ATP can activate the NLRP3 inflammasome and induce IL-1β and chemokines secretion. ATP has anti-bacterial infection effects and can protect mice against bacterial infection in mice.
    ATP-<sup>13</sup>C<sub>10</sub>,<sup>15</sup>N<sub>5</sub>,d<sub>14</sub> (dilithium)
  • HY-168009
    NLRP3-IN-45
    Inhibitor
    NLRP3-IN-45 (D6) is an inhibitor of NLRP3 inflammasome activation, inhibiting the activity of IL-1β (IC50=41.79 nM). NLRP3-IN-45 exerts its effects without affecting the initial stage of NLRP3 inflammasome activation. NLRP3-IN-45 specifically inhibits the activation of NLRP3 inflammasome in the LPS-induced acute lung injury (ALI) mouse model.
    NLRP3-IN-45
  • HY-163498
    NLRP3-IN-37
    Inhibitor
    NLRP3-IN-37 (Compound 23) is a NLRP3 inhibitor (EC50: 5 nM). NLRP3-IN-37 can be used for NLRP3 related research, such as gout, pseudogout, CAPS, NASH fibrosis, heart failure, idiophathic pericarditis, atopic dermatitis, inflammatory bowel disease, Alzheimer's Disease, Parkinson's Disease and traumatic brain injury.
    NLRP3-IN-37
  • HY-133133
    IIIM-1270
    Inhibitor 98.78%
    IIIM-1270is a NLRP3 inflammasome inhibitor. IIIM-1270 inhibits IL-1β release in mouse macrophages (J774A.1 cells) (IC50 = 3.5 μM) and significantly reduced the protein expression level of mature IL-1β. IIIM-1270 can be used for the study of inflammation.
    IIIM-1270
  • HY-173555
    HDAC6-IN-54
    Antagonist
    HDAC6-IN-54 (Compound 9m) is a highly selective HDAC6 (histone deacetylase 6) inhibitor with an IC50 value of 0.021 μM. HDAC6-IN-54 blocks the activation of the NLRP3 inflammasome, which alleviates symptoms of NLRP3 inflammasome-related diseases such as acute peritonitis, inflammatory bowel disease, and psoriasis.
    HDAC6-IN-54
  • HY-183296
    NLRP3-IN-91
    Inhibitor
    NLRP3-IN-91 is a potent NLRP3 inflammasome inhibitor with a Kd of 558.4 nM. NLRP3-IN-91 directly targets the NLRP3 NACHT domain, blocks inflammasome assembly and activation, and exerts anti-inflammatory effects. NLRP3-IN-91 increases survival time in a murine model of LPS (HY-D1056)-induced sepsis. NLRP3-IN-91 can be used for the research of sepsis.
    NLRP3-IN-91
  • HY-156121
    NLRP3-IN-20
    Inhibitor
    NLRP3-IN-20 (compound 11) is an orally available inhibitor of the NLRP3 inflammasome with an IC50 of 25 nM for IL-1β secretion. NLRP3-IN-20 has excellent pharmacokinetic properties and demonstrated significant efficacy in models of non-alcoholic steatohepatitis, fatal septic shock, and colitis.
    NLRP3-IN-20
  • HY-P5523
    iE-DAP
    Agonist
    iE-DAP is a Nod1 agonist. iE-DAP 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 downregulates the expression of ZO-1 and Occludin genes. iE-DAP increases the secretion of IL-6, GRO-α, MCP-1, IL-8 and MIP-1β in term human trophoblast cell cultures. iE-DAP triggers preterm birth in pregnant mice, reduces fetal body weight, and induces fetal inflammation. iE-DAP is applicable to research related to mastitis and preterm birth.
    iE-DAP
  • HY-169227
    NLRP3-IN-55
    Inhibitor
    NLRP3-IN-55 (Compound 19) is a potent NLRP3 inhibitor (IC50 = 0.34 μM). NLRP3-IN-55 directly targets the NLRP3 protein (KD = 0.45 μM), blocking the assembly and activation of the NLRP3 inflammasome, leading to anti-inflammatory effects and inhibition of cellular pyroptosis.
    NLRP3-IN-55
  • HY-183995
    SH-26
    Inhibitor
    SH-26 is a PHD1 PROTAC degrader with DC50s of 1.06 μM, 4.16 μM and 4.91 μM in MDA-MB-231, HepG2 and HEK-293T cells, respectively. SH-26 recruits CRBN to induce PHD1 degradation via the ubiquitin-proteasome system. SH-26 attenuates APAP (HY-66005)-triggered ROS accumulation, mitochondrial dysfunction, and NLRP3 inflammasome activation. SH-26 can be used for the research of acute liver injury.
    SH-26
  • HY-176837
    NOD2/TLR4 agonist-1
    Agonist
    NOD2/TLR4 agonist-1 (Compound 2) is a NOD2/TLR4 dual agonist. NOD2/TLR4 agonist-1 lacks immunostimulatory activity and serves as an important negative control in research.
    NOD2/TLR4 agonist-1
  • HY-183283
    CAII-IN-15
    Inhibitor
    CAII-IN-15 is a potent carbonic anhydrase II (CA II) inhibitor with a hCA II IC50 of 10 nM. CAII-IN-15 elevates cGMP levels, releases nitric oxide, reduces oxidative stress, and exhibits neuroprotective activity in vitro. CAII-IN-15 inhibits NLRP3 inflammasome activation, reduces neuronal apoptosis. CAII-IN-15 reduces Intraocular pressure (IOP) in rabbits. CAII-IN-15 can be used for the research of glaucoma.
    CAII-IN-15
  • HY-168024
    NOD1/2-IN-1
    Inhibitor
    NOD1/2-IN-1 (Compound 18) is a potent RIPK2 inhibitor with an IC50 value of 1.4 nM, as determined by the ADP-Glo assay. NOD1/2-IN-1 blocks the production of pro-inflammatory cytokines by inhibiting the NOD1/NOD2 pathways, with IC50 values of 18 nM and 170 nM for NOD1 and NOD2, respectively, thereby reducing inflammatory responses. NOD1/2-IN-1 can be used in studies related to colitis.
    NOD1/2-IN-1
  • HY-N0633R
    Muscone (Standard)
    Inhibitor
    Muscone (Standard) is the analytical standard of Muscone. This product is intended for research and analytical applications. Muscone is the main active monomer of traditional Chinese medicine musk. Muscone inhibits NF-κB and NLRP3 inflammasome activation. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6), and ultimately improves cardiac function and survival rate.
    Muscone (Standard)
  • HY-169188
    NLRP3-IN-50
    Inhibitor
    NLRP3-IN-50 (compound SN3-1) is a potential NLRP3 inhibitor with therapeutic potential for inflammatory diseases..
    NLRP3-IN-50
  • HY-183337
    ZM734
    Inhibitor
    ZM734 is an orally active and selective NLRP3 inflammasome inhibitor. ZM734 inhibits the secretion of IL-1β. ZM734 alleviates pulmonary inflammation in a mouse model of acute lung injury. ZM734 can be used for the research of inflammatory diseases such as acute lung injury.
    ZM734
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