tlr 8

Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.

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

Imiquimod (R 837) is an immune response modifier and a toll-like receptor 7 (TLR7) agonist with antiviral and antitumor effects. It is used in the study of external genital warts, perianal warts, cancer, and COVID-19, and is commonly employed to induce psoriasis models.

Resiquimod (R848) is an agonist of Toll-like receptors 7 and 8 (TLR7/TLR8) that induces the upregulation of cytokines including TNF-α, IL-6, and IFN-α. It possesses immunomodulatory, antitumor, and antiviral activities, and can be used to induce models of myocarditis and systemic lupus erythematosus (SLE).

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

CU-CPT17e is a potent agonist of TLR(TLR3, TLR8, and TLR9).

CL075 (3M002) is a selective TLR8 agonist with immunomodulatory activity, triggering the MyD88-dependent signaling pathway and activating NF-κB and IRF7 to elicit the production of inflammatory cytokines and type I interferon (IFN).

CL097 is an effective agonist of TLR7 and TLR8. CL097 induces pro-inflammatory cytokines in macrophages and NADPH oxidase priming, thereby increasing the fMLF-stimulated ROS production.

BMS-905 is a potent dual inhibitors of TLR7 and TLR8 with good selectivity against TLR9 and other family members. BMS-905 can be used in studies about the treatment of diseases such as psoriasis, arthritis, and lupus.

CU-CPT-9a is a potent TLR8 inhibitor (IC50 : 0.5 nM), that suppresses TLR8-mediated proinflammatory signaling in various cell lines and human primary cells-

Alogliptin Benzoate (SYR 322)(SYR 322), an effective and specific DPP-4 inhibitor (IC50<10 nM), exhibits greater than 10, 000-fold selectivity over DPP-8 9. Alogliptin may inhibit inflammatory responses by preventing the toll-like receptor 4 (TLR-4)-mediated formation of proinflammatory cytokines.

Schaftoside (APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE) has antioxidant and anticancer activity.

Motolimod (VTX-378) (VTX-2337) is an effective and specific Toll-like receptor (TLR) 8 agonist (EC50: 100 nM), > 50-fold selectivity over TLR7.

TLR7 8 agonist 3 is a potent activator of TLR7 and TLR8.

Loxoribine (RWJ 21757) is a guanosine analog. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist. It has anti-viral and anti-tumor activities.Loxoribine is a potent new immunostimulant with a relatively broad spectrum of immunobiological activities.

Telratolimod (MEDI9197) is a toll-like receptors 7 8 agonist. It has an antitumor activity.

AYK004 is an adenosine derivative that functions as a TLR7 8 agonist, enhancing immune responses by activating the TLR signaling pathway. It boasts an optimal hydrophilic-lipophilic balance, improving its loading rate and stability within immunoadjuvant systems like liposomes, and reduces the side effects of these systems during systemic immunization.

UM-3006 is a potent TLR7 8 agonist that enhances immune responses by activating the TLR signaling pathway. This compound holds significant research and application potential in the fields of vaccine adjuvants and immune diseases.

3M-003 interacts with Toll-like receptor-7 (TLR-7) and TLR-8. 3M-003 acts directly on macrophages to enhance fungal killing and stimulates PBMC to produce soluble factors that enhance killing by neutrophils, macrophages, and monocytes. 3M-003 could be a candidate for antifungal immunotherapy.

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

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.

TLR7/8 agonist 4 hydroxy-PEG10-acid [compound 9] is a drug-linker conjugate used in antibody-drug conjugates (ADC), exhibiting remarkable antitumor activity. It utilizes TLR7/8 agonist 4, a potent activator of TLR7/8, linked to hydroxy-PEG10-acid via a cleavable bond, demonstrating promising pharmaceutical potential in ADC-based therapeutics.

TLR7/8 agonist 4 TFA (compound 41) is a highly potent TLR7/8 agonist demonstrating significant anti-cancer activity.

TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugate used in antibody-drug conjugates (ADCs) with high tumor efficacy. It consists of TLR7/8 agonist 4, a potent TLR7/8 agonist, linked to the ADC linker hydroxy-PEG10-acid, which can be cleaved.