Toll-like Receptor (TLR) Inhibitor

rel-TLR4-IN-2 (Compound 13) is a biologically active indane compound with anti-inflammatory activity. rel-TLR4-IN-2 exerts anti-inflammatory effects by inhibiting the TLR4 signaling pathway. rel-TLR4-IN-2 can be used for the research of inflammatory diseases.

ODN INH-1 sodium is palindromic and a class R (‘restricted’) inhibitory ODN. ODN INH-1 sodium is a potent inhibitor of TLR9-induced B cells and macrophages

Pamidronic acid sodium, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronic acid sodium significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of osteoprotegerin in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronic acid sodium can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.

TLR3 Human Pre-designed siRNA Set A contains three designed siRNAs for TLR3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

ENDO12 is an inhibitor of the Munc13-4-STX7 protein complex, with a K_d value of 2.7 µM for STX7. ENDO12 blocks the interaction of Munc13-4-STX7. ENDO12 inhibits endolysosomal flux, endolysosomal cargo degradation, the extracellular signal-regulated kinase signaling pathway in neutrophils, the IFN regulatory factor signaling pathway in plasmacytoid dendritic cells, and the responses of primary dendritic cells to TLR3, TLR7, and TLR9. ENDO12 alleviates CpG-induced systemic inflammation by reducing the levels of myeloperoxidase, IL-6 and IFNγ. ENDO12 does not interfere with the host's antiviral response to lymphocytic choriomeningitis virus infection.\nENDO12 can be used in studies related to systemic inflammation.

TLR7/8 agonist 9 (Compound 25a) is a TLR7/8 agonist, with EC₅₀s of 40 nM and 23 nM for hTLR7/8. TLR7/8 agonist 9 has anti-tumor activity and improves the antitumor activity of PD-1/PD-L1 blockade. TLR7/8 agonist 9 can be used for research of cancer immunotherapy.

Trimebutine-d₃ hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

Juglone (Standard) is the analytical standard of Juglone. This product is intended for research and analytical applications. Juglone (5-hydroxy-1,4-naphthalenedione) is a yellow dye that can be extracted from Juglans regia. Juglone induces apoptosis through the mitochondrial pathway. Juglone has antibacterial and antitumor activity .

JM-9 is a inhibitor of MD2. JM-9 suppresses high glucose and palmitic acid -induced inflammation in MPMs. JM-9 improves diabetic kidney disease by inhibiting MD2-mediated inflammation.

Famotidine-¹³C,d₃ (MK-208-¹³C,d₃) is the deuterated, ¹³C-labeled Famotidine (HY-B0377). Famotidine (MK-208) 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 inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine 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 crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer.

Lytx-Pa2a (Lycotoxin-Pa2a) is a peptide inhibitor against bacterial membranes and TLR4 receptor. Lytx-Pa2a exerts antimicrobial effects via non-competitive disruption of outer/cytoplasmic membranes and suppression of LPS-induced TLR4/NF-κB signaling. Lytx-Pa2a is promising for research of bacterial infection and inflammation-related disease (e.g., sepsis).

Anti-TLR7 Antibody is a CHO-expressed human antibody that targets TLR7. Anti-TLR7 Antibody contains huIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Anti-TLR7 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).

Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

Trimebutine-d₅ fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

HCN-IN-1 is a TLR4 inhibitor and HCN channel modulator with activity against HCN2 and HCN4.HCN-IN-1 inhibits TLR4-mediated alkaline phosphatase (SEAP) signal activity.HCN-IN-1 reduces HCN2 current across tested voltages, shifts voltage-dependent activation to more hyperpolarized potentials, slows activation kinetics, and does not affect deactivation process.HCN-IN-1 blocks HCN4 current.HCN-IN-1 exhibits analgesic, anti-inflammatory, and anti-anginal effects.HCN-IN-1 can be used for the research of inflammatory pain, neuropathic pain, heart failure, inflammation.

Papiliocin is a potent peptide antibiotic with both anti-inflammatory and antibacterial activities. Papiliocin is primarily active against Gram-negative bacteria. Papiliocin exhibits strong anti-inflammatory activity against cell, exerting its anti-inflammatory activity by inhibiting the production of NO and the secretion of TNF-α and MIP-2. Papiliocin participates in the innate defense response mechanism by inhibiting the Toll-like receptor pathway and NF-κB. Papiliocin induces apoptosis in fungal cells and increases the total level of intracellular ROS. Papiliocin acts as an effective antiseptic peptide in sepsis models. Papiliocin is useful in anti-inflammatory and antibacterial research.

BIM-46174 is a heterotrimeric G protein complex inhibitor. BIM-46174 blocks GPCR downstream signaling by trapping Gα proteins in a nucleotide-free pocket conformation, thereby inhibiting Gαq-mediated calcium release, Gαs-mediated cAMP production, and GPCR-regulated cancer cell invasion. In vitro, BIM-46174 effectively suppresses a variety of clinically multidrug-resistant cell lines and induces tumor cell apoptosis through activation of caspase-3 and PARP cleavage. BIM-46174 also inhibits activation of the Neu1-MMP-9-GPCR signaling platform and downstream NF-κB signaling, and is widely used in the study of cancer signaling pathways and inflammation-related research, including lung cancer, pancreatic cancer, breast cancer, melanoma, and leukemia.

Anti-CD14 Antibody (UCHM-1) reacts with the human CD14. Anti-CD14 Antibody (UCHM-1) recognizes a cell surface glycoprotein expressed on most peripheral blood monocytes. Recommend Isotype Controls: Mouse IgG2a kappa, Isotype Control (HY-P99978).

Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

5-Chloroisoquinoline (compound 42) is an inhibitor of SARM1 (Sterile alpha and toll/interleukin receptor (TIR) motif containing protein 1), an enzyme involved in axon degeneration that catalyzes multiple activities through a ternary complex mechanism. 5-Chloroisoquinoline can be used in the study of neurodegenerative diseases or axon degeneration.