Toll-like Receptor (TLR) Inhibitor

Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₅₀=1.13 μM).

Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-α and IL-6 production with IC_50s 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.

Chymotrypsin (EC 3.4.21.1; Chymotrypsin A) (MS grade) is an orally effective inhibitor targeting molecules such as TLR4, NF-κB, MMP-1, TNF-α, IL-1β, and IL-6. Chymotrypsin (MS grade) downregulates the TLR4/NF-κB signaling pathway, inhibits the release of inflammatory factors, reduces cell infiltration and tissue damage, and also reduces the expression of tumor cell adhesion molecules (such as CD44 and CD54). It can also be specifically detected by fluorescent probes (such as NBD-3). Chymotrypsin (MS grade) has anti-inflammatory, hepatoprotective, joint damage-reducing, liver protection against lipotoxicity, and anti-tumor metastasis functions, and can be used in the research of diseases such as rheumatoid arthritis, non-alcoholic fatty liver disease, and melanoma metastasis. Chymotrypsin (MS grade) can be used in studies of inflammation, edema, and expectoration.

NB-7 is a substituted pyridine derivative and SARM1 inhibitor. NB-7 can be used for the research of neurological disorders.

Hydroxychloroquine (HCQ) is a synthetic oral antimalarial drug that can be used in the study of malaria and autoimmune diseases such as systemic lupus erythematosus and rheumatoid arthritis. Hydroxychloroquine is a potent autophagic flux inhibitor with antiviral activity (such as SARS-CoV-2 virus) that inhibits Toll-like receptor 7/9 (TLR7/9) signaling.

Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₅₀=1.13 μM).

C29 is a Toll-like receptor 2 (TLR2) inhibitor. C29 blocks hTLR2/1 and hTLR2/6 signaling with IC₅₀s of 19.7 and 37.6 μM, respectively.

Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC₅₀s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .

Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.

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.

Chymotrypsin (EC 3.4.21.1; Chymotrypsin A) is an orally effective inhibitor targeting molecules such as TLR4, NF-κB, MMP-1, TNF-α, IL-1β, and IL-6. Chymotrypsin downregulates the TLR4/NF-κB signaling pathway, inhibiting the release of inflammatory factors, reducing cell infiltration and tissue damage. It also reduces the expression of tumor cell adhesion molecules (such as CD44 and CD54) and can be specifically detected by fluorescent probes (such as NBD-3). Chymotrypsin has anti-inflammatory, hepatoprotective, joint damage-reducing, liver protection against lipotoxicity, and anti-tumor metastasis functions. It can be used in research on diseases such as rheumatoid arthritis, non-alcoholic fatty liver disease, and melanoma metastasis. Chymotrypsin can be used in studies of inflammation, edema, and expectoration.

Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab is used in the study of hypercholesterolemia and atherosclerotic cardiovascular disease. Evolocumab binds to circulating PCSK9 protein and inhibits its binding to LDLR. Evolocumab has antioxidant and cytoprotective activities against H₂O₂-induced oxidative damage to endothelial cells. Evolocumab may also negatively regulate activation of the TLR-4/NF-κB signaling pathway to prevent inflammation.

Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.Thiamine hydrochloride activates NrF-2/HO-1 and inhibits TLR4, NF-κB. Thiamine hydrochloride has neuroprotective and anti-inflammatory effects. Thiamine hydrochloride can be used in the studys of diabetic complications, neurological diseases, cancers, and colitis.

IRF5-IN-1 (Compound C5) is a conformationally locked inhibitor for SLC15A4. IRF5-IN-1 blocks the downstream IRF5 activation, inhibits the TLR7/8 signaling pathway. IRF5-IN-1 exhibits anti-inflammatory responses.

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.

DSRM-3716 (5-Iodoisoquinoline) is a potent and selective SARM1 NADase inhibitor with an IC₅₀ of 75 nM. DSRM-3716 is selective against other NAD⁺-processing enzymes, receptors, and transporters. DSRM-3716 provides robust axon protection.

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.

TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.

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

ABR-238901 is an orally active and potent S100A8/A9 blocker and inhibits S100A8/A9 interaction with its receptors RAGE (receptor for advanced glycation endproducts) and TLR4 (toll-like receptor 4). ABR-238901 has the potential for myocardial infarction (MI) research.