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.

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-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.

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.

TQL-1055 is a semi-synthetic analog of the saponin adjuvant QS-21 (HY-101092) and can be used as a prophylactic vaccine adjuvant. TQL-1055 exhibits robust adjuvant activity for influenza antigens. TQL-1055 combined with the acellular pertussis vaccine (aP) shows good tolerance and enhances the antibody response to pertussis toxin (PT) in mice and rabbits. TQL-1055 is promising for research of chronic hepatitis B.

QS 7 (QS 7 Api) is a saponin compound that can be extracted from the Quillaja saponaria tree. QS 7 activates immune cells, enhances their antigen presentation ability and cytokine secretion. QS 7 can be used as vaccine adjuvant for immunostimulating, anti-tumor, and anti-infectious activities.

QS-21, an immunostimulatory saponin, could be used as a potent vaccine adjuvant. QS-21 stimulates Th2 humoral and Th1 cell-mediated immune responses through action on antigen presenting cells (APCs) and T cells. QS-21 can activate the NLRP3 inflammasome with subsequent release of caspase-1 dependent cytokines, IL-1β and IL-18[1][2][3].

AYK004-B1 is a TLR7 agonist (EC50=0.2265 nM). AYK004-B1 can be used to prepare immune adjuvants.

AYK004 is a TLR7/8 agonist that enhances immune responses by activating the TLR signaling pathway. AYK004 is an adenine derivative with a favorable hydrophilic-lipophilic balance, which improves the loading capacity and stability in immunoadjuvant systems such as liposomes, while reducing the side effects of the immunoadjuvant system in systemic immunity .

AYK005 is a TLR7/8 immunologic adjuvant.

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

3D-Monophosphoryl Lipid A-5 (3D-MPLA-5) is a TLR agonist that can be used as an adjuvant for vaccines to enhance their immunogenicity.

3D-Monophosphoryl Lipid (12,16) (3D-MPL (12,16)) free acid is a TLR agonist that can be used as a vaccine adjuvant to enhance the immunogenicity of vaccines[1].
