Toll-like Receptor (TLR) Inhibitor

Liriodendrin is an orally effective lignan compound with anti-inflammatory, antioxidant, and anti-platelet aggregation activities. Liriodendrin is isolated and extracted from Sargentodoxae caulis and Linaria vulgaris. Liriodendrin regulates the expression of genes related to inflammation and cellular metabolism by inhibiting the NF-κB, PI3K/Akt, and TLR4 signaling pathways, or by activating the PI3K-DDX18 pathway. Liriodendrin increases the expression of HSF1 and HSP27 without cytotoxicity. Liriodendrin is used in studies on ulcerative colitis, myocardial ischemia-reperfusion injury, sepsis-induced acute lung injury, and chronic endometritis.

Saquinavir (Standard) (Ro 31-8959 (Standard)) is the analytical standard of Saquinavir (HY-17007). This product is intended for research and analytical applications. Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells.

6-Methoxyflavone (Standard) is the analytical standard of 6-Methoxyflavone (HY-W097625). This product is intended for research and analytical applications. 6-Methoxyflavone is an orally active methoxyflavone. 6-Methoxyflavone suppresses neuroinflammation in microglia through the inhibition of TLR4/MyD88/p38 MAPK/NF-κB dependent pathways and the activation of HO-1/NQO-1 signaling. 6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway and activates the PERK/EIF2a/ATF4/CHOP pathway in HeLa cells. 6-Methoxyflavone acts as a Flumazenil (HY-B0009)-insensitive positive allosteric modulator at human recombinant α1β2γ2L and α2β2γ2L GABAα receptors. 6-Methoxyflavone inhibits NFAT Translocation into the nucleus and suppresses T cell activation. 6-Methoxyflavone partially restores chronic ethanol-induced behavioral deficits in mice. 6-Methoxyflavone antagonizes chronic constriction injury and diabetes associated neuropathic nociception expression. 6-Methoxyflavone can be used for the study of cancer, inflammation and neurological diseases.

TLR4-IN-2 (Compound Racemic-11k) is inhibitors of TLR4, JNK, and NF-κB. TLR4-IN-2 inhibits NO production in LPS-stimulated RAW264.7 cells with an IC₅₀ value of 23.2 µM. TLR4-IN-2 exerts anti-inflammatory activity by inhibiting TLR4 expression, reducing JNK phosphorylation, thereby suppressing the activation of NF-κB, blocking the transcription of inflammation-related genes, reducing the expression of iNOS and COX-2, and decreasing the production of inflammatory mediators such as NO, PGE 2, and TNF-α. TLR4-IN-2 is promising for research of inflammatory diseases, such as rheumatoid arthritis and various inflammatory disorders.

Isoacteoside (Standard) is the analytical standard of Isoacteoside. This product is intended for research and analytical applications. Isoacteoside is a natural product that can significantly inhibit the formation of glycation end products. Isoacteoside Standard regulates the AKT/PI3K/m-TOR/NF-κB signaling pathway, induces apoptosis in OVCAR-3 cell. Isoacteoside Standard exhibits antitumor, anti-inflammatory, anti-obesity and neuroprotective activities.

Famotidine hydrochloride (MK-208 hydrochloride) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine hydrochloride inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine hydrochloride scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine hydrochloride crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine hydrochloride reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine hydrochloride can be used in studies related to COVID-19, liver injury and acute gastric ulcer.

Poseltinib (Standard) is the analytical standard of Poseltinib (HY-109010). This product is intended for research and analytical applications. Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine K_inase (BTK) inhibitor. With an IC₅₀ of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis.

Ecliptasaponin A (Standard) is the analytical standard for Ecliptasaponin A (HY-N1508). Ecliptasaponin A is an orally active pentacyclic triterpenoid saponin. Ecliptasaponin A exerts anti-tumor activity by activating ASK1/JNK pathway, inducing apoptosis and autophagy in lung cancer cells. Ecliptasaponin A exerts anti-inflammatory/anti-fibrotic effects and protects the cardiovascular system by inhibiting the HMGB1/TLR4/NF-κB pathway, and the expression of COX-2 and MMP-9. Ecliptasaponin A can enhance SOD activity, reduce MDA levels, and alleviate oxidative stress damage. Ecliptasaponin A exerts chondroprotective effects by inhibiting the expression of MMP13 and regulating inflammatory factors. Ecliptasaponin A improves ovarian function and regulates sex hormones by upregulating the expression of ESR1 receptors.

CU-CPT 4a (Standard) is the analytical standard of CU-CPT 4a (HY-108473). This product is intended for research and analytical applications. CU-CPT 4a (TLR3-IN-1) is a potent, highly selective TLR3 signaling inhibitor. CU-CPT 4a represses the expression of downstream signaling pathways mediated by the TLR3/dsRNA complex, including TNF-α and IL-1β.

ODN 21595 sodium is a Guanine-Modified TLR7 and TLR9 inhibitor. ODN 21595 sodium inhibits the release of IFN-α and IL-6 with no cytotoxic. ODN 21595 sodium reduces the expression of CD86 and HLA-DR. ODN 21595 sodium has the potential for the research of systemic lupus erythematosus (SLE).

Hecubine is a monoterpene indole alkaloid found in Ervatamia ocinalis. Hecubine activates TREM2 expression, reduces LPS (HY-D1056)-stimulated inammatory cytokines (TNF-α、IL-6、IL-1β) overexpression, as well as suppresses the levels of TLR4-, MyD88-, MAPK/PI3K/AKT- and NF-κB-related proteins. Hecubin also exhibits antioxidative effect, reduces ROS production and activates of the Nrf2/HO-1 pathway. Hecubine rescues LPS-induced behavioral deficits in zebrash larvae. Hecubine can be used for the research of neural inflammation-associated central nervous system diseases.

Resatorvid (Standard) is the analytical standard of Resatorvid (HY-11109). This product is intended for research and analytical applications. Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-α and IL-6 production with IC₅₀s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases.

TLR4-IN-C34 (Standard) is the analytical standard of TLR4-IN-C34 (HY-107575). This product is intended for research and analytical applications. TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.

N-(p-Coumaroyl) Serotonin (Standard) is the analytical standard of N-(p-Coumaroyl) Serotonin (HY-129440). This product is intended for research and analytical applications. N-(p-Coumaroyl) Serotonin is an orally active polyphenol found in safflower seeds with potent anti-inflammatory, antioxidant, and antitumor activities. N-(p-Coumaroyl) Serotonin suppresses NF‑κB, TLR4/MyD88 and MAPK signaling, activates NQO1/HO‑1 pathways, and inhibits pro‑inflammatory cytokines, iNOS and COX‑2 and ROS production. N-(p-Coumaroyl) Serotonin induces S‑phase arrest and apoptosis in glioblastoma cells, reduces atherosclerotic lesions, and alleviates renal and vascular injuries. N-(p-Coumaroyl) Serotonin acts as a vasodilator, regulates calcium dynamics. N-(p-Coumaroyl) Serotonin can be used for the research of neurodegenerative diseases, atherosclerosis, glioblastoma, and acute renal failure.

Phellopterin (Standard) is the analytical standard of Phellopterin. Phellopterin, an orally active furocoumarin with multiple biological activities. Phellopterin is a partial agonist of the central benzodiazepine receptors. Phellopterin exerts anti-inflammatory effects by upregulating SIRT1, downregulating ICAM-1 (reducing chronic inflammation, aiding diabetic ulcer healing), inhibiting STAT3 phosphorylation (easing atopic dermatitis inflammation), regulating Akt/PKC pathways (lowering TNF-α-induced VCAM-1 to block monocyte adhesion), and inhibiting TLR4/NF-κB pathway and macrophage M2 polarization (alleviating colitis-related cancers). Phellopterin suppresses ovarian cancer progression via inhibiting the PU.1/CLEC5A/PI3K-AKT loop (inducing cell cycle arrest, apoptosis, DNA damage). Phellopterin alleviates murine diabetes by promoting adipocyte differentiation and increasing PPARγ. Phellopterin also has anti-HSV-1 activity. Phellopterin can be used for studying anti-inflammation, anti-cancer (e.g., ovarian cancer, colitis cancer), blood glucose lowering, anti-diabetes, and anti-virus.

Robinin (Standard) is the analytical standard of Robinin. This product is intended for research and analytical applications. Robinin is a flavonoid that can be extracted from the leaves of purple cowpea, inhibiting TGF-β, TLR4/NF-κB and TLR2-PI3k-AKT signaling pathways. Robinin exerts anti-inflammatory and anti-tumor effects. The combination of Robinin and Methotrexate (HY-14519) reduces inflammation in experimental arthritis, Robinin can decrease the Doxorubicin (HY-15142A) induced cardiac toxicity effect.

Schaftoside (Standard) is the analytical standard of Schaftoside. This product is intended for research and analytical applications. Schaftoside is a flavonoid found in a variety of Chinese herbal medicines, such as Eleusine indica. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.

Antibacterial agent 284 (Compound 7) is an Antibacterial agent. Antibacterial agent 284 has a zinc-binding structure and potent inhibitory activity against Legionella pneumophila metalloprotease ProA (IC₅₀: 0.96 μM) with zinc-binding structure. Antibacterial agent 284 significantly inactivates the cleavage of collagen IV and flagellin (ProA substrates) and reduces immune evasion from the TLR5-NF-κB pathway and PMN-mediated inflammation in human lung tissue explants. Antibacterial agent 284 is promising for Legionnaires' disease research.

IMG-2005 is a TLR signaling pathway inhibitor. IMG-2005 mimics the Toll/interleukin-1 receptor (TIR) domain of MyD88, thereby preventing its homodimerization, which causes damage to tracheal epithelial cells and triggers pulmonary immune diseases.

CU-CPT22 (Standard) is the analytical standard of CU-CPT22 (HY-108471). This product is intended for research and analytical applications. CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a K_i of 0.41 µM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC₅₀ of 0.58 µM.