TLR8 agonist 5 is a potent TLR8 agonist with an EC50 value of 20 nM for HEK-Blue hTLR8. TLR8 agonist 5 activates the immune response[1].
Resatorvid (TAK-242) is a potent TLR4 signaling inhibitor which selectively inhibits the TLR4-mediated production of cytokines and nitric oxide.
Cobitolimod is a DNA oligonucleotide agonist of TLR-9 with anti-inflammatory activity. Cobitolimod suppresses Th17 cells and induces anti-inflammatory FoxP3 and IL-10 expression, inhibiting the IL-17 signaling pathway[1].
Kdo2-Lipid A ammonium is a chemically defined lipopolysaccharide (LPS) with endotoxin activity equal to LPS. Kdo2-Lipid A ammonium is highly selective for TLR4. Kdo2-Lipid A ammonium stimulates the release of both TNF and PGE2[1].
TLR7 agonist 4 (Compound 1.2) is a TLR7 agonist with an EC50 of 4.3 nM[1].
Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.
GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for the treatment of asthma[1].
AN-3485 is a benzoxaborole analog, Toll-Like Receptor(TLR) inhibitor with IC50 values ranging from 18 to 580 nM.
6'-Sialyllactose is a sialylated human milk oligosaccharide that can promote the proliferation of bifidobacteria and shaping the gut microbiota. 6'-Sialyllactose also inhibits toll-like receptor 4 signaling and protects against the development of necrotizing enterocolitis[1][2].
ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'[1][2].
Diprovocim is a potent Toll-like receptor TLR1/TLR2 agonist that induces dose-dependent TNF production with EC50 of 110 pM in human THP-1 cells and 1.3 nM in primary mouse peritoneal macrophages; induces TNF production in bone marrow-derived dendritic cells (BMDC) with EC50 of 6.7 nM, also induces IL-6 production by mouse BMDC; induces phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα in THP-1 cells and mouse peritoneal macrophages, activates conventional TLR1/TLR2 signaling, including MAPK and canonical NF-κB signaling; synergizes with anti-PD-L1 to eliminate melanoma in mice.
TLR7/8 agonist 1 dihydrochloride is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.
IAXO-102 is a TLR4 antagonist, inhibits MAPK and p65 NF-kB phosphorylation involved in down regulation of the expression of TLR4 and TLR4 dependent proinflammatory protein. IAXO-102 prevents experimental abdominal aortic aneurysm development[1].
Lefitolimod (MGN 1703) is a DNA-based TLR9 agonist and an immune surveillance reactivator. Lefitolimod induces HIV-specific immune responses and can be used for the research of cancer and HIV-1[1][4].
TLR4-IN-C34-C2-COO 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[1].
TLR7 agonist 9 (compound 10) is an aonist of TLR7. TLR7 agonist 9 can be used for research of cancer and infectious disease[1].
Ruzotolimod is the agonist of TLR7. Ruzotolimod has the potential for the research of HBV, COVID-19 or SARS-CoV-2 infection (extracted from patent WO2021130195A1)[1].
Paridiprubart (NI-0101) is a humanised anti-TLR4 monoclonal antibody. Paridiprubart has the potential for the research of rheumatoid arthritis[1].
MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate[1].
C29 is a Toll-like receptor 2 (TLR2) inhibitor.
MAPK-IN-1 (Compound 2) is a MAPK signaling pathway inhibitor. MAPK-IN-1 exhibits AChE inhibitory activity with an IC50 of 23.84 μM. MAPK-IN-1 shows anti-neuroinflammatory and neuroprotective activity and can be used for Alzheimer's disease research[1].
Desethyl chloroquine diphosphate is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine diphosphate possesses antiplasmodic activity[1][2].
AXC-715 hydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1[1]. AXC-715, compound D from WO2020190734A1, can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants[2].
TLR7 agonist 6 (compound IIb-19) is an TLR7 agonist with an EC50 value of ~4 nM[1].
ODN 24991, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR3, TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 24991 disrupts TLR3-, TLR7- and TLR9-mediated immune cell immune responses. ODN 24991 sequence: 5'-C-C-T-G-G-C-c7rGm-G-G-G-3'[1].
CU CPT 4a is a potent inhibitor of the toll-like receptor 3 (TLR3)/double-stranded RNA (dsRNA) complex. CU CPT 4a shows dose-dependent inhibitory effects blocking Poly (I:C)-induced TLR3 activation with an IC50 of 3.44 µM[1][2].
TLR7/8-IN-1 is a crystalline from of a TLR7/TLR8 inhibitor extracted from patent WO2019220390, compound 2b. TLR7/8-IN-1 can be used for the research of autoimmune disease[1].
ODN 24987 is a Guanine-modified inhibitory oligonucleotides (ODN), targeting TLR9. ODN 24987 can inhibit IL-6 and IFN-α release. ODN 24987 can be used for research immune disorders. ODN 24987 sequence: 5’-C-C-T-G-G-C-c7G-G-G-G-3’[1].
CU-CPT-9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM.
BMS-905 is a potent dual inhibitor of TLR7 and TLR8 with IC50 of 0.3 nM (TLR7, IL-6 inhibition in mouse blood), shows good selectivity against TLR9 and other TLR family members.