| DC47326 |
TLR3-IN-1 |
CU CPT 4a is a potent inhibitor of the toll-like receptor 3 (TLR3)/double-stranded RNA (dsRNA) complex. CU CPT 4a shows dose-dependent inhibitory effects blocking Poly (I:C)-induced TLR3 activation with an IC50 of 3.44 µM. |
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| DC48179 |
Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH |
Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis. |
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| DC48180 |
GSK1795091 |
GSK1795091 (CRX-601), an immunologic stimulator, is a synthetic TLR4 agonist. Antitumor activity. GSK1795091 can be used as a vaccine adjuvant to enhance both mucosal and systemic immunity to influenza virus vaccines. |
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| DC48181 |
Polvitolimod |
Polvitolimod is a TLR7 agonist for treatment of cancer and infectious disease. |
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| DC48182 |
Poly(I:C) |
Poly(I:C) is a synthetic double-stranded RNA (dsRNA), which is a Toll-like receptor 3 (TLR3) agonist. Poly(I:C) present in some viruses, and is therefore commonly used to model the actions of extracellular dsRNA. |
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| DC48183 |
Ruzotolimod |
Ruzotolimod is the agonist of TLR7. Ruzotolimod has the potential for the research of HBV, COVID-19 or SARS-CoV-2 infection (extracted from patent WO2021130195A1). |
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| DC48184 |
TLR7/8 agonist 4 TFA |
TLR7/8 agonist 4 TFA (compound 41) is a potent TLR7/8 agonist. TLR7/8 agonist 4 has anti-cancer activity. |
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| DC48724 |
AXC-715 trihydrochloride
Featured
|
AXC-715 trihydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1. AXC-715 trihydrochloride, compound D from WO2020190734A1, can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants. |
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| DC49403 |
β-D-Glucan |
β-D-glucan is a natural non-digestible polysaccharide and high biocompatibility that can be selectively recognized by recognition receptors such as Dectin-1 and Toll-like receptors as well as being easily internalized by murine or human macrophages, which is likely to attribute to a target delivery. β-d-glucan is an enteric delivery vehicle for probiotics. |
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| DC49674 |
TLR7/8 agonist 6 |
TLR7/8 agonist 6 (Compound 4) is the potent agonist of TLR7/8 with IC50s of 0.18 and 5.34 μM, respectively. TLR7/8 agonist 6 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders. |
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| DC49676 |
SM-360320 |
SM-360320 (CL-087) is a potent, oral actively TLR7 agonist. SM-360320 is a mmuno-modulator and exerts an antitumor effect. SM-360320 can act in synergy with DNA vaccines leading to an enhanced Th1 antibody response. SM-360320 can inhibit HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity. |
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| DC49677 |
DB-3-291 |
DB-3-291 is potent and selective CSK degrader, with a Kd of 1 nM. |
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| DC49678 |
TLR7/8 antagonist 2 |
TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases. |
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| DC49679 |
TLR7/8 antagonist 1 |
TLR7/8 Antagonist 1 (Compound 16c) is the potent antagonist of TLR7/8 with IC50s of 3.91 and 2.19 μM, respectively. TLR7/8 Antagonist 1 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders. |
|
| DC70264 |
BMS-905 |
BMS-905 is a potent dual inhibitor of TLR7 and TLR8 with IC50 of 0.3 nM (TLR7, IL-6 inhibition in mouse blood), shows good selectivity against TLR9 and other TLR family members. |
|
| DC70330 |
CU-72 |
CU-72 is a potent, selective TLR7/8 dual inhibitor with IC50 of 5.10 and 2.87 uM, respectively. |
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| DC70332 |
CU-CPD107
Featured
|
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. |
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| DC70786 |
SM360320 |
SM360320 (CL-087, 1V136) is a potent, orally active and selective TLR7 agonist (ligand).SM360320 inhibited HCV replication in Huh-7 cells in a dose-dependent manner in the Huh-7 replicon system, reduced HCV mRNA and protein levels in isolated Huh-7 hepatocytes.SM360320 induced in vivo secretion of interferon alpha (IFNalpha) and exerted a significant antitumor effect in CEA.Tg mice challenged with a syngenic tumor cell line expressing CEA.SM360320 exerts significant antitumor effects and can act in association with DNA-EP for CEA-positive colon cancer and HER2-positive mammary carcinoma.Repeated low dose administration of SM360320 induced hyporesponsiveness or tolerance to TLR2, -7, and -9 activators and limited the course of neural inflammation in an experimental allergic encephalomyelitis model. |
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| DC71126 |
TL8-506 |
TL8-506 is a specific TLR8 agonist with an EC50 of 30 nM. TL8-506 can be used for the research of tuberculosis and autoimmune diseases. |
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| DC71529 |
UC-1V150 |
UC-1V150 is a specific TLR7 (Toll-like receptor) agonist that stimulates cellular immune responses and has anti-tumor activity. UC-1V150 can be used to synthesize ISAC (Immune-Stimulating Antibody Conjugates) molecule. |
|
| DC71530 |
Agatolimod |
Agatolimod (ODN 2006), a class B ODN (oligodeoxynucleotide), is a TLR9 agonist. Agatolimod is also an optimal CpG sequence for humans. Agatolimod stimulates very strong production of NO2 and IL-6 in HD11 cells. Agatolimod can be used for breast cancer research. Sequence: 5'-tcgtcgttttgtcgttttgtcgtt-3'. |
|
| DC71531 |
ODN 1826 |
ODN 1826, a class B ODN (oligodeoxynucleotide), is a TLR9 agonist. CpG ODN 1826 is an excellent immunostimulator that induces NO and iNOS production in the murine model. CpG ODN 1826 enhances cell apoptosis. ODN 1826 sequence: 5’-tccatgacgttcctgacgtt-3’. |
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| DC71785 |
CL097 hydrochloride |
CL097, a potent TLR7 and TLR8 agonist, induces pro-inflammatory cytokines in macrophages. CL097 induces NADPH oxidase priming, resulting in an increase of the fMLF-stimulated ROS production. |
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| DC71786 |
ODN 2395 |
ODN 2395 is a C class oligodeoxynucleotide and can be used as vaccine adjuvant. ODN 2395 is also a TLR9 agonist. Sequence: 5'-tcgtcgttttcggcgc:gcgccg-3'. |
|
| DC71787 |
ODN 24888 |
ODN 24888 is an guanine-modified inhibitory oligonucleotides (INH-ODN), shows potent inhibition on TLR7/TLR9-mediated signaling. ODN 24888 impairs IFN-α level and NF-κB activation, inhibits IL-6 release. ODN 24888 involves in immune and inflammatory responses, can be used as a vaccine adjuvant. |
|
| DC71788 |
ODN 24991 |
ODN 24991, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR3, TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 24991 disrupts TLR3-, TLR7- and TLR9-mediated immune cell immune responses. ODN 24991 sequence: 5'-C-C-T-G-G-C-c7rGm-G-G-G-3'. |
|
| DC71789 |
ODN D-SL01 |
ODN D-SL01, a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. ODN D-SL01 has strong immunostimulatory activity in a variety of vertebrate species and has anticancer activity. ODN D-SL01 sequence: 5'- T-C-G-C-G-A-C-G-T-T-C-G-C-C-C-G-A-C-G-T-T-C-G-G-T-A-3'. |
|
| DC71790 |
ODN M362 |
ODN M362, a class C oligodeoxynucleotide, is a TLR-9 agonist and can be used as a vaccine adjuvant. ODN M362 induces cancer cell apoptosis. |
|
| DC71791 |
ODN TTAGGG |
ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'. |
|
| DC72352 |
TMX-201 |
TMX-201 is a TLR7 ligand-phospholipid conjugate. TMX-201 shows potent immune stimulatory activity. TMX-201 can be used for breast cancer and melanoma research. |
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