TLR

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

CU-T12-9 is a potent TLR1/2 agonist(EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay).

IAXO-102 is a TLR4 antagonist that negatively regulates TLR4 signaling.

BMS-905 is a potent dual inhibitors of TLR7 and TLR8 with good selectivity against TLR9 and other family members.

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

CU-CPT22: first TLR1/2 complex probe, binds at TLR1/2 interface (IC50=0.58μM), inhibits Pam3CSK4 binding (Ki=0.41μM).

TLR7 agonist 17 (compound 20) functions as a highly effective TLR7 agonist, exhibiting EC 50 values of 12 nM for hTLR7 and 17 nM for mTLR7. Additionally, this compound has demonstrated anticancer activity [1].

PTD-N5-1 (N5-1) is an IRF5 inhibitory peptide. It can block the production of IL-12 induced by β-glucan in both wild-type and Clec2d-deficient bone marrow-derived dendritic cells (BMDC) that are activated by IFN-γ. PTD-N5-1 modulates antifungal immunity by inhibiting IRF5-mediated IL-12 production.

TLR8 agonist8 (Compound II-72) is an agonist of Toll-like receptor 8 (TLR8) with an EC50 of 0.25-1 μM. It demonstrates stability in both human and mouse plasma and induces the secretion of the cytokine TNFα with an EC50 of less than 1 μM. In the MC38-HER2 xenograft mouse model, TLR8 agonist8 exhibits antitumor activity, achieving a tumor growth inhibition (TGI) rate of 89%.

TLR2antagonist-1 is a selective antagonist of Toll-like receptor 2 (TLR2). It effectively inhibits excessive activation of TLR2, with an IC50 value of 11.41 μM, and reduces the production of inflammatory factors. TLR2antagonist-1 exhibits metabolic stability, with a half-life (T1/2) of 16.67 minutes in mouse liver microsomes. This compound is useful for research in inflammation, immunology, and neurological disorders.

MTvkPABC-P5d TFA, a TLR7 agonist, functions as an immune stimulant. It is applicable in the synthesis of immune-stimulating antibody conjugates (ISAC).

TLR7 agonist21 (Compound 27B) is a selective activator of Toll-like receptor 7 (TLR7), with an EC50 of 17.53 nM for human TLR7 and 41.7 nM for mouse TLR7. It induces the secretion of pro-inflammatory cytokines, including IL-6, TNF-α, IFN-α1, and IL-4. Acting as a vaccine adjuvant, TLR7 agonist21 enhances IgG and IgA levels, offering protection for mice against influenza virus infection.

Lipopolysaccharides from Klebsiella pneumoniae (LPS, from bacterial [Klebsiella pneumoniae]) are lipid-polysaccharide endotoxins and TLR4 activators originating from Klebsiella pneumoniae, classified as S-type LPS. They exhibit a characteristic tripartite structure comprising an O-antigen, a core oligosaccharide, and lipid A. These lipopolysaccharides may contribute to bacterial immune evasion by inhibiting complement-mediated killing and suppressing host antimicrobial peptide secretion, thus helping bacteria evade immune defenses. Possessing high viscosity and serum resistance, they can potentially induce sepsis. Additionally, these lipopolysaccharides are utilized in the development of animal models for sepsis/septicemia.

TLR8 agonist7 is an agonist of Toll-like receptor 8 (TLR8) with an EC50 of less than 250 nM. It remains stable in human and mouse plasma and induces the secretion of the cytokine TNFα with an EC50 of less than 1 μM. In the MC38-HER2 xenograft mouse model, TLR8 agonist7 demonstrates antitumor activity, achieving a tumor growth inhibition (TGI) rate of 98%.

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MTT5, a toll-like receptor 7 (TLR7) agonist, can be conjugated with Deruxtecan to exert antitumor activity in HER2-positive solid tumors through tumor cell killing and immune activation.

Pam3CSK4-Biotin is a biotinylated derivative of Pam3CSK4, functioning as a Toll-like receptor 1/2 (TLR1/2) agonist.

TLR2/6 agonist; boosts TNF-α in human cells & mouse B cell growth/activation.

CRX 527 is a TLR4 ligand and serves as an adjuvant for peptide cancer vaccines, enhancing anti-tumor immune responses. CRX 527 also induces hematopoietic stem cell (HSC) differentiation, increasing the proportion and number of LSK cells, and promotes their differentiation into macrophages. This activation bolsters immune defense and protects intestinal epithelium from radiation damage.

TLR7/8 agonist 12 (compound 9) is a human TLR7/8 agonist with EC50 values of 11 nM for hTLR7 and 150 nM for hTLR8, indicating its potential for immune modulation.