TLR-1

TLR1 is a cell-penetrating Toll IL-1 receptor resistance (TIR) domain BB-Loop mimic and inhibits IL-1 receptor-mediated responses.

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

Pam3CSK4 TFA (Pam3Cys-Ser-(Lys)4 TFA) is a Toll-like receptor 1 2 agonist with EC50 of 0.47 ng mL for human TLR1 2.

C29 is a novel inhibitor of TLR2 1 and TLR2 6 signaling induced by synthetic and bacterial TLR2 agonists in human HEK-TLR2 and THP-1 cells, but only TLR2 1 signaling in murine macrophages.

TLR7 agonist 2 (TLR7-IN-1) is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM).

CU-CPT9b (TLR8-specific antagonist 1) is an antagonist of toll-like receptor 8 (TLR8; Kd = 21 nM). It inhibits activation of NF- B induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells with an IC50 value of 0.7 nM.

1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist known for its anti-tumor properties.

STAMBP-IN-1 is a novel selective antagonist of deubiquitinase STAM-binding protein (STAMBP), decreasing NALP7 protein levels and suppressing IL-1β release after TLR agonism.

MD2-TLR4-IN-1 is a myeloid differentiation protein 2 toll-like receptor 4 (MD2-TLR4) complex inhibitor.

TLR7 agonist 1 is a selective and oral TLR7 agonist (IC50: 90 nM).

CU-CPT22 is the first probe for the complex between toll-like receptors TLR1 and TLR2. CU-CPT22 binds at the interface of TLR1 and TLR2 (IC50 = 0.58 μM). It competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1 2 (Ki: 0.41 μM).

Gardiquimod is a TLR7 8 agonist. When used at concentrations below 10 μM, Gardiquimod specifically activates TLR7. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells.

4-Octylphenol is an endocrine disruptor with gender-specific effects on male germ cells, significantly reducing the mitotic index and the number of spermatogonia. It also causes inflammatory damage in the gills of carp by activating the complement system through the C3a C3a receptor (C3a C3aR) axis and C5a C5a receptor 1 (C5a C5aR1) axis. Furthermore, 4-Octylphenol induces immune suppression by disrupting the balance between helper T (Th) cells 1 Th2 and regulatory T (Treg) Th17 cells, and triggers inflammatory damage through the Toll-like receptor 7 (Toll-like Receptor (TLR)) inhibitor κBα nuclear factor κB (TLR7 IκBα NF-κB) pathway.

TLR3-IN-1 (CU CPT 4a) is a selective TLR3 inhibitor (IC50: 3.44 μM in RAW 264.7 cells). It can inhibit TLR3 dsRNA complex-mediated downstream signaling pathways and inhibit the production of TNF-α and IL-1β in whole cells.

The Immuno-Oncology Screening Library consists of 2 plates and contains more than 90 cancer and immunology-associated compounds in a 96-well Matrix tube rack format as 10 mM stock solutions in DMSO. This library includes a variety of immuno-oncology target modulators, including but not limited to, adenosine, CCR, CXCR, and TLR agonists and antagonists, BTK, PI3K, VEGFR, and BRAF inhibitors, PD-1/PDL-1 interaction inhibitors, and HDAC inhibitors. Please review the product insert for a full list of targets. Stability data is not available for the compounds as supplied in the screening library.

Givinostat (ITF-2357) is an HDAC inhibitor with IC50 values of 198 nM for HDAC1 and 157 nM for HDAC3.

TLR7 8-IN-1, a crystalline TLR7 TLR8 inhibitor from patent WO2019220390 (compound 2b), is a valuable compound for autoimmune disease research.

TLR7 8 9-IN-1 is a potent inhibitor of Toll-like receptors 7, 8, and 9 (TLR7 8 9) with an IC50 of 43 nM.

MD2-IN-1 is a Myeloid differentiation protein 2 (MD2) inhibitor with a KD of 189  μM for the recombinant human MD2 (rhMD2).

TLR7 8 agonist 1 dihydrochloride (TLR7 8 agonist-5d) is a TLR7 8 agonist which shows prominent immunostimulatory activities.

TLR7 8 Antagonist 1 (Compound 16c), an imidazoquinoline derivative, is a potent TLR7 8 agonist with IC50 values of 3.91 and 2.19 μM for TLR7 and TLR8, respectively. rel-O-2050 (TLR-2050) is a key target for drug development in infectious diseases, cancer, and autoimmune diseases.

L6H21 is an MD-2 inhibitor that can be used to study cognitive impairment and brain damage.

1. Ginsenoside Rg5 could be a beneficial agent for the treatment of Alzheimer's disease. 2. Ginsenoside Rg5 suppresses LPS-induced nitric oxide (NO) production and proinflammatory TNF-α secretion. 3. Ginsenoside Rg5 can ameliorate lung inflammation possib

MyD88-IN-1 is a potent MyD88 inhibitor with anti-inflammatory activity, inhibiting downstream pathways such as the NF-κB pathway of the Toll-like receptor (TLR) and interleukin-1 (IL-1) receptor family. MyD88-IN-1 may be used in the study of cancer and inflammation treatment.