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-170233
    NLRP3-IN-75
    		Inhibitor
    NLRP3-IN-75 is an orally active NLRP3 inhibitor. NLRP3-IN-75 suppresses IL-1β secretion (IC50 = 23 nM). NLRP3-IN-75 selectively inhibits NLRP3 activation by disrupting inflammasome assembly without affecting NLRC4 or AIM2 inflammasomes. NLRP3-IN-75 exhibits superior efficacy in acute peritonitis, diabetic kidney disease and IBD models.
    NLRP3-IN-75
  • HY-177128
    Sebrinoflast
    		Inhibitor
    Sebrinoflast (Compound 5) is a NLRP3 inhibitor with an IC50 ≤1  μM for hNLRP3. Sebrinoflast can be used for inflammatory and cardiovascular diseases including NASH and atherosclerosis and neurological diseases like Alzheimer's disease research.
    Sebrinoflast
  • HY-163300
    NLRP3-IN-30
    		Inhibitor
    NLRP3-IN-30 (Compound A14) is a potent NLRP3 inhibitor, with an IC50 of 44.43 nM. NLRP3-IN-30 has highly oral bioavailability (F is 83.09% in mice).
    NLRP3-IN-30
  • HY-155762
    Anti-neuroinflammation agent 1
    		Inhibitor
    Anti-neuroinflammation agent 1 is a potent anti-neuroinflammation agent that regulates polarization BV2 microglia cells from M1 phenotype to M2 phenotype.
    Anti-neuroinflammation agent 1
  • HY-CE00479
    (6Z,9Z,12Z,15Z,18Z,21Z)-Tetracosahexaenoyl-CoA
    		Modulator
    (6Z,9Z,12Z,15Z,18Z,21Z)-Tetracosahexaenoyl-CoA ((6Z,9Z,12Z,15Z,18Z,21Z)-Tetracosahexaenoyl-coenzyme A) is a NLRX1 modulator. (6Z,9Z,12Z,15Z,18Z,21Z)-Tetracosahexaenoyl-CoA is promising for research of immune and metabolic related diseases.
    (6Z,9Z,12Z,15Z,18Z,21Z)-Tetracosahexaenoyl-CoA
  • HY-159928
    Neuroprotective agent 8
    		Inhibitor
    Neuroprotective agent 8 (compound AA-9) is an oral active neuroprotective agent by anti-oxidative stress and anti-inflammation. Neuroprotective agent 8 activates PGC-1α and inhibits NLRP3 in the rat MCAO ischemic stroke model.
    Neuroprotective agent 8
  • HY-B0516A
    Articaine
    		Inhibitor
    Articaine (Hoe-045) 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 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 can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury).
    Articaine
  • HY-182051
    HDAC3 degrader-2
    		Inhibitor
    HDAC3 degrader-2 is a selective HDAC3 degrader. HDAC3 degrader-2 inhibits the activation of the NLRP3 inflammasome by degrading HDAC3, thereby reducing the maturation of IL-1β and caspase-1. HDAC3 degrader-2 exhibits anti-inflammatory activity. HDAC3 degrader-2 can be used in research related to endotoxin shock, colitis and gouty arthritis.
    HDAC3 degrader-2
  • HY-118316
    GSK223
    		Inhibitor
    GSK223 is a quinazolinone NOD1 pathway inhibitor with potential anti-inflammatory activity. GSK223 can selectively inhibit IL-8 release under iE-DAP stimulation without affecting IL-8 secretion caused by TNF receptor, TLR2 or NOD2 agonists. GSK223 does not directly inhibit RIP2 kinase activity.
    GSK223
  • HY-163494
    NLRP3-IN-36
    		Inhibitor
    NLRP3-IN-36 (Compound 111) is an NLRP3 inhibitor (IC50 <1 μM).
    NLRP3-IN-36
  • HY-N6712R
    Thiolutin (Standard)
    		Inhibitor
    Thromycin (Standard) is the analytical standard of thromycin (Acetopyrrothin) (HY-N6712). Thiolutin is a sulfur-containing antibiotic, which is a potent inhibitor of bacterial and yeast RNA polymerases. Thiolutin can be produced by Streptomyces. Thiolutin inhibits AMSH (IC50 = 4 μM) and Rpn11 (IC50 = 0.53 μM). Thiolutin is a dual inhibitor of BRCC36 and the NLRP3 inflammasome, exhibiting anti-inflammatory effects. Thiolutin effectively suppresses the interaction between BRCC36 and HMGCR, leading to the inhibition of HCC growth. Thiolutin attenuates pyroptosis and NLRP3 inflammasome activation. Thiolutin markedly alleviates renal injury and inflammatory process in IgAN. Thiolutin is an anti-angiogenic compound which can ease Doxorubicin (HY-15142A)-induced cardiotoxicity (DOXIC)[1][2][3][4][5].
    Thiolutin (Standard)
  • HY-17355BS
    Dexpramipexole-d3 dihydrochloride
    		Inhibitor
    Dexpramipexole-d3 ((R)-Pramipexole-d3) dihydrochloride is the deuterium labeled Dexpramipexole. Dexpramipexole ((R)-Pramipexole) 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-d<sub>3</sub> dihydrochloride
  • HY-15193R
    EMD638683 (Standard)
    		Inhibitor
    EMD638683 (Standard) is the analytical standard of EMD638683. This product is intended for research and analytical applications. EMD638683 is an orally effective SGK1 inhibitor with an IC50 of 3 μM. EMD638683 exhibits strong inhibition against SGK1, moderate inhibition against SGK2 and SGK3, and shows excellent selectivity for other AGC kinase family members. EMD638683 has antihypertensive activity by inhibiting SGK1, and independently of the blood pressure-lowering effect, it effectively prevents heart inflammation and fibrosis caused by hypertension by inhibiting the cardiac NLRP3 inflammation body/ IL-1β axis. EMD638683 promotes apoptosis of colon cancer cells and sensitizes radiotherapy. EMD638683 (S-Form) can be used in research related to hypertension, hypertensive heart damage, and colon cancer.
    EMD638683 (Standard)
  • HY-110051
    DPP4-In hydrochloride
    DPP4-In (hydrochloride) is an inhibitor of dipeptidyl peptidase 4 (DPP4) that can reduce DPP4 expression.
    DPP4-In hydrochloride
  • HY-100573R
    Necrosulfonamide (Standard)
    		Inhibitor
    Necrosulfonamide (Standard) is the analytical standard of Necrosulfonamide (HY-100573). This product is intended for research and analytical applications. Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.
    Necrosulfonamide (Standard)
  • HY-N2485R
    4'-Methoxyresveratrol (Standard)
    		Activator
    4'-Methoxyresveratrol (Standard) is the analytical standard of 4'-Methoxyresveratrol. This product is intended for research and analytical applications. 4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation.
    4'-Methoxyresveratrol (Standard)
  • HY-N0589R
    Dehydrodiisoeugenol (Standard)
    		Inhibitor
    Dehydrodiisoeugenol (Standard) is the analytical standard of Dehydrodiisoeugenol (HY-N0589). This product is intended for research and analytical applications. Dehydrodiisoeugenol is an orally active anti-inflammatory and anti-tumor agent. Dehydrodiisoeugenol inhibits the proliferation of colorectal cancer cells, and induces apoptosis, autophagy, endoplasmic reticulum stress and cell cycle arrest. Dehydrodiisoeugenol also exerts anti-inflammatory effects by inhibiting the activation of NF-κB and the expression of COX-2. Dehydrodiisoeugenol can be used in the research related to colorectal cancer, inflammatory diseases and ulcerative colitis.
    Dehydrodiisoeugenol (Standard)
  • HY-N0257R
    Epimedin A (Standard)
    		Inhibitor
    Epimedin A (Standard) is the analytical standard of Epimedin A (HY-N0257). This product is intended for research and analytical applications. Epimedin A, one of the main flavonoid active components in Herba Epimedii, is orally active. Epimedin A can inhibit osteoclastogenesis, differentiation, and bone resorption. Epimedin A also possesses anti-inflammatory activity. Epimedin A can be used in the research of osteoporosis and inflammatory diseases.
    Epimedin A (Standard)
  • HY-B0116A
    Stavudine sodium
    		Inhibitor
    Stavudine (d4T) sodium is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine sodium has activity against HIV-1 and HIV-2. Stavudine sodium also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine sodium reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine sodium induces apoptosis.
    Stavudine sodium
  • HY-W741136
    (R)-Colchicine
    		Inhibitor
    (R)-Colchicine is the R-isomer of Colchicine (HY-16569). Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research.
    (R)-Colchicine
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
NOD-like Receptor (NLR) Isoform Comparison

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