CU-CPT-8m is a nolve TLR8 inhibitor.

ODN4084-F is a class B (‘broadly-active’) inhibitory ODN. ODN 4084-F is potent inhibitor of TLR9-induced B cells and macrophages.

ODN 2395 is a C class oligodeoxynucleotide and can be used as vaccine adjuvant. ODN 2395 is also a TLR9 agonist. Sequence: 5'-tcgtcgttttcggcgc:gcgccg-3'.

ODN 1826, a class B ODN (oligodeoxynucleotide), is a TLR9 agonist. CpG ODN 1826 is an excellent immunostimulator that induces NO and iNOS production in the murine model. CpG ODN 1826 enhances cell apoptosis. ODN 1826 sequence: 5’-tccatgacgttcctgacgtt-3’.

ODN D-SL01, a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. ODN D-SL01 has strong immunostimulatory activity in a variety of vertebrate species and has anticancer activity. ODN D-SL01 sequence: 5'- T-C-G-C-G-A-C-G-T-T-C-G-C-C-C-G-A-C-G-T-T-C-G-G-T-A-3'.

RS 09 is a TLR4 agonist. RS 09 promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 acts as an adjuvant in vivo; RS 09 enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.

CU-CPD107 is a TLR8-specific small molecule with unique synergistic agonist activities in the presence of ssRNA, but inactive without the aid of ssRNA.CU-CPD107 significantly inhibited of R848-induced signaling in HEK-Blue hTLR8 cells with an IC50 of 13.7 uM.CU-CPD107 only inhibited synthesized small-molecule agonist-induced TLR8 signaling without affecting other TLRs.CU-CPD107 synergistically increased IFN-β, TNF-α, IL-1β, IL-6, and IL-8 mRNA expression levels in the presence of 5 μg/ml ssRNA40 in HEK-Blue hTLR8 cells, whereas CU-CPD107 alone did not. CU-CPD107 only activated TLR8-mediated signaling in the presence of ssRNA.CU-CPD107 showed no pure agonistic activity, addressing a major challenge that has existed for previous TLR7 and TLR8 agonists as vaccine adjuvants or antiviral drugs.

C29 is a potential TLR2 inhibitor.

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 asthma.

Monophosphoryl lipid A (Glucopyranosyl lipid A) is a toll-like receptor 4 agonist. Monophosphoryl lipid A is derived from the cell wall of nonpathogenic Salmonella. Monophosphoryl lipid A can be used for the research of immunization and vaccine.

Polyinosinic-polycytidylic acid (Poly(I:C)) sodium is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis.

Sulfo-ara-F-NMN (CZ-48) is a mimetic of nicotinamide mononucleotide (NMN). Sulfo-ara-F-NMN acts selectively, activating SARM1 but inhibiting CD38 (IC50 around 10 μM). Sulfo-ara-F-NMN induces intracellular cyclic ADP-ribose (cADPR) production.

Pam3CSK4 TFA is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2.

TAK-242 (Resatorvid), a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4.

AXC-715 trihydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1. AXC-715 trihydrochloride, 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.

SZU-106 is a small molecule TLR7 agonist, selectively activates TLR7 and increases the expression of SEAP by activating the NF-κB pathway.

SZU101 is a small molecule TLR7 agonist that directly activates, induces reporter activity (23-fold) in a TLR7-NF-kB reporter system expressed in HEK-293 cells TLR7 signalling.

MHV370 (MHV-370) is a potent, selective, orally bioavailable inhibitor of Toll-like receptors 7 and 8 (TLR7/8) with IC50 of 1.1 and 4.5 nM in cell-based assays.

E567 is a small moleculeTLR2 signaling inhibitor with anti-viral activity, efficiently inhibits both LCMV and HSV-1 induced cytokine responses in both human and mouse cell cultures.

Diprovocim-X is a potent human and murine TLR1/TLR2 agonist with EC50 of 0.14 nM (hTLR1/TLR2) and 0.75 nM (m TLR1/TLR2), respectively.

AZD8848 (AZD 8848) is a potent, selective TLR7 agonist with EC50 of 4 nM for induction of IFNα from human PBMCs and an IC50 of 0.2-1.0 nM for inhibition of IL-5.

ODN 5328 (ODN 2395 Control) can be used as a sequence control for C-class ODN 2395. ODN 5328 shares the sequence with ODN 2395 but contain GpC dinucleotides instead of the CpG motifs.

Enpatoran (M5049) hydrochloride is a potent, orally active, and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM, respectively, in HEK293 cells.

RDR 02308 is a TLR4-MyD88 binding inhibitor that inhibits full-length β-lactamase.

CU-CPT9b is an antagonist of toll-like receptor 8 (TLR8; Kd = 21 nM).

TMX-201 is a TLR7 ligand-phospholipid conjugate. TMX-201 shows potent immune stimulatory activity. TMX-201 can be used for breast cancer and melanoma research.

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'.

ODN M362, a class C oligodeoxynucleotide, is a TLR-9 agonist and can be used as a vaccine adjuvant. ODN M362 induces cancer cell apoptosis.

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'.

ODN 24888 is an guanine-modified inhibitory oligonucleotides (INH-ODN), shows potent inhibition on TLR7/TLR9-mediated signaling. ODN 24888 impairs IFN-α level and NF-κB activation, inhibits IL-6 release. ODN 24888 involves in immune and inflammatory responses, can be used as a vaccine adjuvant.