C29 is a potential TLR2 inhibitor.

Chloroquine diphosphate is an antimalarial drug and autophagy/lysosome inhibitor; inhibits Toll-like receptor (TLR) signalling in plasmacytoid dendritic cells (pDCs).

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

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

CU-CPT9a is an antagonist of toll-like receptor 8 (TLR8). It inhibits activation of NF-κB induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells (IC50 = 0.5 nM). CU-CPT9a reverses R-848-induced increases in NF-κB p65, IRAK-4, and TRAF3 protein levels in HEK-Blue cells.

Isatoribine is a selective agonist of TLR7

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.

TLR7 and 8 modulator 31 is a potent, orally active, dual TLR7 and 8 agonist with LEC values of 0.15 and 0.16 uM, respectively.

Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist.

DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect.

CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.

1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity.

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.

TLR7/8 agonist 3 is a potent TLR7 and TLR8 agonist, extracted from patent US20170114137A1.

Polyinosinic-polycytidylic acid sodium (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.

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

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

Pam3CSK4-Biotin is biotinylated Pam3CSK4. Pam3CSK4-Biotin is a Toll-like receptor 1/2 (TLR1/2) agonist.

MMG-11 quarterhydrate is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 quarterhydrate inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7?μM for Pam3CSK4-induced hTLR2/1 and 5.7?μM for Pam2CSK4-induced hTLR2/6 responses.

Sparstolonin B acts as a selective TLR2 and TLR4 antagonist and selectively blocks TLR2- and TLR4-mediated inflammatory signaling. Sparstolonin B has anti-HIV and anticancer activities.

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.

Chitohexaose hexahydrochloride is a chitosan oligosaccharide with anti-inflammatory effect. Chitohexaose hexahydrochloride binds to the active sites of TLR4 and inhibits LPS induced inflammation.