SMU-R39 is a TLR7 and TLR8 antagonist with IC50 values of 3.22 μM and 0.24 μM, respectively. SMU-R39 binds to recombinant mTLR7 protein (KD = 2.36 μM) and to recombinant hTLR8 protein (KD = 105 nM). SMU-R39 suppresses downstream NF-κB and MAPK signaling, and reduces secretion/transcription of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in PBMCs and THP-1 cells. SMU-R39 demonstrates anti-inflammatory efficacy in Imiquimod (IMQ)-induced psoriasis mouse model. SMU-R39 can be used for the study of autoimmune diseases such as psoriasis.

GlcNAc-MurNAc, a disaccharide, is a TLR4 agonist with a Kd of 383 μM for murine TLR4. GlcNAc-MurNAc directly binds to TLR4 and activates its downstream NF-κB and IRF pathways. GlcNAc-MurNAc improves Dextran sulfate sodium salt (DSS)-induced colitis in mice through a TLR4-dependent mechanism. GlcNAc-MurNAc can be used for the study of inflammatory bowel disease.

GNE-5152 is an orthosteric SARM1 base-exchange (BE) inhibitor. GNE-5152 sustainably activates SARM1 at subinhibitory concentrations under mildly activating conditions, and this synergistic adverse effect increases NAD consumption, induces axon degradation and neurodegeneration and releases neurofilament-light (NfL) in cortical neurons. GNE-5152 can be used for neurodegenerative diseases research.

NB-3 is a nicotinamide adenine dinucleotide (NAD) hydrolase SARM1 inhibitor. NB-3 intercepts NAD hydrolysis and undergoes covalent conjugation with the reaction product adenosine diphosphate ribose (ADPR). The resulting small-molecule ADPR adducts are highly potent and confer compelling neuroprotection in neurological injury.

TLR4L 10 is a TLR4 ligand. TLR4L 10 induces cells to produce IL-6. TLR4L 10 has immunostimulatory activity.

L07-2 (Compound 6) is an active scaffold comprising a stimulator of TLR7/8. L07-2 can be used for synthesis of immune-stimulating antibody conjugates (ISACs) for cancers research.

(Rac)-VB-201 is the racemate of VB-201, an oxidized phospholipid small molecule that inhibits CD14- and toll-like receptor 2-dependent innate cell activation and suppresses atherosclerosis.

APG-7 binds to the TLR4/MD-2 interface, thereby inhibiting NO production (IC50 of 24.2 μg/mL). APG-7 is an Apigenin derivative. APG-7 has low toxicity to the 3T3 fibroblast cell line. APG-7 can be used for the study of oxidative stress and inflammation.

SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits  MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8+T cells. SMU-L11-R shows potential in colorectal cancer studies.

ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research.

CCL-34 is a Toll-like receptor 4 (TLR4) activator. CCL-34 significantly induced dendritic cell (DC) CD83 expression and IL-12p70 production in a dose-dependent manner, thereby inducing DC maturation. CCL-34 enhanced the allostimulatory activity of DC on naive CD4+CD45+RA+ T cell proliferation and IFN-γ secretion. CCL-34 further induced antigen presentation ability in mice inoculated with doxorubicin-treated colorectal cancer cells. CCL-34 can be used in studies of immune stimulation.

E-5531 is an endotoxin antagonist. E-5531 quickly becomes inactive after binding with HDL. E-5531 can block the Toll like receptor 4 (TLR4) signaling pathway. E-5531 can be used for the study of endotoxemia and septic shock.

SMU-C68 is a highly selective small-molecule TLR1/2 heterodimer agonist (EC50=0.009 μM). SMU-C68 activates NF-κB and MAPK pathways to promote pro-inflammatory cytokine release (e.g., TNF-α, IL-1β). SMU-C68 is promising for research of cancers.

ETI41 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.63 μM) and TLR9 (IC50 = 0.16 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI41 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI41 can be used for autoimmune and inflammatory diseases research.

DSP30 is a phosphorothioate cpG-oligodeoxynucleotide and a TLR9 agonist. DSP30 can activate immune system cells, including B cells and dendritic cells, by inducing proliferation and cytokine production.DSP30 can enhance the immunosuppressive function of bone marrow-multipotent mesenchymal stromal cells (BM-MSC). DSP30 combined with interleukin 2 (IL2) is an effective mitotic stimulant in B-cell disorders. DSP30 can be used for the genetic characteristic research and analysis of chronic lymphocytic leukemia (CLL).

Sitmutolimod, a CpG oligonucleotide, is a Toll-like receptor agonist with antineoplastic activity.

Sitmutolimod sodium, a CpG oligonucleotide, is a Toll-like receptor agonist with antineoplastic activity.

Rintatolimod is a Toll-like receptor 3 (TLR-3) agonist. It has dual impact on restraining PDAC cell functions and boosting the antitumor immune response.

Nelitolimod, a CpG oligonucleotide, is a TLR9 agonist.

Nelitolimod sodium, a CpG oligonucleotide, is a TLR9 agonist.

Litenimod is potent type B agonist of toll Like receptor 9 (TLR9), triggering both innate and adaptive immune response.

Litenimod sodium is potent type B agonist of toll Like receptor 9 (TLR9), triggering both innate and adaptive immune response.

GNKG168 is a synthetic, 21-mer, unmethylated CpG oligodeoxynucleotide. It acts as a TLR9 agonist with immunostimulatory activity.

GNKG168 sodium is a synthetic, 21-mer, unmethylated CpG oligodeoxynucleotide. It acts as a TLR9 agonist with immunostimulatory activity.

CpG-ODN c41, an oligonucleotide, is an antagonist of TLR9.

CpG-ODN c41 sodium, an oligonucleotide, is an antagonist of TLR9.

Bazlitoran, an oligonucleotide, is an antagonist of TLR7, TLR8, and TLR9.

Bazlitoran sodium, an oligonucleotide, is an antagonist of TLR7, TLR8, and TLR9.

SMU-14a is a TLR3 inhibitor (IC50: 0.18 µM). SMU-14a inhibits IL-6 secretion in mouse peritoneal macrophages and downregulates TNF-α in human peripheral blood monocytes. SMU-14a exerts anti-inflammatory effects by reducing the phosphorylation of p65, ERK, and TBK1 through NF-κB, MAPK, and IRF3 signaling pathways, and decreasing serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. SMU-14a can be used in the study of acute hepatitis.

Pixatimod free acid (PG545 free acid) is a mimetic of Heparan Sulfate. 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats.