Telratolimod (MEDI 9197, 3M 052) is a novel, injectable, tissue-retained TLR7/8 agonist that forms a tissue depot with gradual, sustained release, allowing local TLR triggering activity without systemic cytokine release.

SMU127 (SMU-127, ZINC666243) is a specific TLR1-TLR2 small molecule agonist with EC50 of 0.55 uM.

A potent TLR7/8 agonist that induces robust production of the Th1-polarizing cytokines TNF-alpha and IL-12 from neonatal antigen-presenting cells (APCs)..

A selective TLR8 agonist that induces activation of NF-κB at 0.4 uM.

3M-011 is a potent TLR7/8 agonist and cytokine inducer; stimulates type I interferon (IFN) and other cytokines such as TNF-alpha, IL-12, and IFN-gamma from rat peripheral blood mononuclear cells; induces IL-12 and COX-2 expression in mDC from HIV+ and HIV- individuals, and inhibits H3N2 influenza viral replication in the nasal cavity; potentiates NK cytotoxicity, and shows antitumor effects in scid/B6 mice and scid/NOD mice.

ANA975 is an oral prodrug of the TLR-7 agonist Isatoribine (ANA245.

CU115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU 115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells.

Novel TLR7 agonist via immune response induction and tumor microenvironment modulation

Toll-like receptor 2/6 (TLR-2/6) agonist, regulating Lcn2 gene, promoting collateral growth

Novel anticryptosporidial agent, acting as a toll-like receptor-2 (TLR2) antagonist

E6742 (E6742) is a potent, selective, dual TLR7/8 inhibitor with binding Kd of 1.7 uM/37 nM in ITC assays, respectively, inhibits TLR7/8 agonist CL097 induced reporter activation with IC50 values of 22, 68, and 3.0 nM for hTLR7, mTLR7, and hTLR8, respecti

Novel potent TLR1/2 Specific Agonist, Suppressing Leukemia Cancer Cell Growth by Stimulating Cytotoxic T Lymphocytes

CL097, a potent TLR7/8 agonist, induces pro-inflammatory cytokines in macrophages. CL097 induces NADPH oxidase priming, resulting in an increase of the fMLF-stimulated ROS production.

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.

AZ617 is a potent TLR4 agonist.

Gardiquimod is a TLR7 agonist, inducing the activation of NF-B in HEK293 cells expressing human or mouse TLR7.

TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis[1][2].

TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88 to interfere with its homodimerization, and the TLR/MyD88 signal pathway. TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI).

Paquinimod is a S100A9 inhibitor, which prevents S100A9 binding to TLR-4.

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.

activate TLR8-dependent NF-kB signaling

E014 is a potent, selective TLR7 agonist with EC50 of 69 nM in Ramos Blue reporter assays, >500-fold selective for TLR7 over TLR8.

CU-CPT17e shows strong NF-κB activation in TLR3, TLR8 and TLR9 HEK293 cells with EC50 values of 4.80±0.73, 13.5±0.58 and 5.66±0.17 μM, respectively. CU-CPT17e significantly improves the activity with 13.9±0.9 fold of NF-κB activation and an EC50 value of 4.8±0.7 μM. CU-CPT17e inhibits the proliferation of HeLa cancer cells by triggering apoptosis and arresting the cell cycle at the S phase. The induction of apoptosis by CU-CPT17e in HeLa cells is investigated. HeLa cells are cultured with increasing concentrations of CU-CPT17e or poly I:C or blank control (DMSO) for 24 h. Treatment with CU-CPT17e for 24 h at different concentrations (10 to 40 μM) results in an elevation of apoptotic cell population ranging from 10% to 17%, which is more effective than poly I:C at 5 μg/mL. These results suggest that the antiproliferative activity of CU-CPT17e against HeLa cells might result from its ability to directly induce apoptosis[1].

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.

D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50=24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2.

TLR7-IN-1 is a novel TLR7 inhibitor.

M1002 is a first-in-class HIF-2a agonists.

C29 is a potential TLR2 inhibitor.

AYK004-C1 is a TLR agonist. AYK004-C1 can be used to prepare immune adjuvants.

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.