| DC22934 |
3M-011
Featured
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3M-011 is a potent TLR7/8 agonist and cytokine inducer; stimulates type I interferon (IFN) and other cytokines such as TNF-alpha, IL-12, and IFN-gamma from rat peripheral blood mononuclear cells; induces IL-12 and COX-2 expression in mDC from HIV+ and HIV- individuals, and inhibits H3N2 influenza viral replication in the nasal cavity; potentiates NK cytotoxicity, and shows antitumor effects in scid/B6 mice and scid/NOD mice. |
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| DC22922 |
3M-003
Featured
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A potent TLR7/8 agonist that induces robust production of the Th1-polarizing cytokines TNF-alpha and IL-12 from neonatal antigen-presenting cells (APCs).. |
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| DC22924 |
3M-002
Featured
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A selective TLR8 agonist that induces activation of NF-κB at 0.4 uM. |
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| DC23543 |
ANA975
Featured
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ANA975 is an oral prodrug of the TLR-7 agonist Isatoribine (ANA245. |
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| DC10276 |
C29
Featured
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C29 is a potential TLR2 inhibitor. |
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| DC26031 |
Gardiquimod trifluoroacetate
Featured
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Gardiquimod trifluoroacetate is a specific TLR7 agonist which can also inhibit HIV-1 reverse transcriptase. |
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| DC7138 |
GS-9620(Vesatolimod)
Featured
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GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7(TLR-7) in chimpanzees with chronic HBV infection. |
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| DC8815 |
Motolimod (VTX-2337)
Featured
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Motolimod (VTX-2337) is a novel TLR8 agonist that activates NK cells and augments ADCC. |
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| DC10875 |
Paquinimod
Featured
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Paquinimod is a S100A9 inhibitor, which prevents S100A9 binding to TLR-4. |
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| DC12437 |
SMU127
Featured
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SMU127 (SMU-127, ZINC666243) is a specific TLR1-TLR2 small molecule agonist with EC50 of 0.55 uM. |
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| DC7733 |
Tasquinimod(ABR-215050)
Featured
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Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. |
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| DC21273 |
Telratolimod
Featured
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Telratolimod (MEDI 9197, 3M 052) is a novel, injectable, tissue-retained TLR7/8 agonist that forms a tissue depot with gradual, sustained release, allowing local TLR triggering activity without systemic cytokine release. |
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| DC10653 |
TLR7-IN-1
Featured
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TLR7-IN-1 is a novel TLR7 inhibitor. |
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| DC28230 |
Loxoribine
Featured
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Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist. |
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| DC28351 |
1V209(TLR7 agonist T7)
Featured
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1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity. |
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| DC28386 |
GSK2245035
Featured
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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. |
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| DC28692 |
TLR7/8 agonist 3
Featured
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TLR7/8 agonist 3 is a potent TLR7 and TLR8 agonist, extracted from patent US20170114137A1. |
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| DC31025 |
TLR4-IN-C34
Featured
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TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis[1][2]. |
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| DC31070 |
M1002
Featured
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M1002 is a first-in-class HIF-2a agonists. |
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| DC34454 |
Gardiquimod
Featured
|
Gardiquimod is a TLR7 agonist, inducing the activation of NF-B in HEK293 cells expressing human or mouse TLR7. |
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| DC42507 |
CU-115
Featured
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CU115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU 115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells. |
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| DC42749 |
AZ617
Featured
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AZ617 is a potent TLR4 agonist. |
|
| DC44159 |
Enpatoran
Featured
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Enpatoran (M5049) is an orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran can block both innate and adaptive autoimmunity. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran (M5049) can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran (M5049) inhibits cytokine release, causing great potency in pharmacokinetic/pharmacodynamic properties. |
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| DC45281 |
RS 09
Featured
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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. |
|
| DC47256 |
TJ-M2010-5
Featured
|
TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88 to interfere with its homodimerization, and the TLR/MyD88 signal pathway. TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI). |
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| DC47884 |
TLR4-IN-C34-C2-COOH
Featured
|
TLR4-IN-C34-C2-COO 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. |
|
| DC48021 |
CL097
Featured
|
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. |
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| DC48401 |
TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride
Featured
|
TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugate for ADC with potent antitumor activity by using TLR7/8 agonist 4, linked via the cleavable ADC linker hydroxy-PEG10-acid.
|
|
| DC49675 |
D18
Featured
|
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. |
|
| DC50032 |
CU-CPT17e
Featured
|
CU-CPT17e shows strong NF-κB activation in TLR3, TLR8 and TLR9 HEK293 cells with EC50 values of 4.80±0.73, 13.5±0.58 and 5.66±0.17 μM, respectively. CU-CPT17e significantly improves the activity with 13.9±0.9 fold of NF-κB activation and an EC50 value of 4.8±0.7 μM. CU-CPT17e inhibits the proliferation of HeLa cancer cells by triggering apoptosis and arresting the cell cycle at the S phase. The induction of apoptosis by CU-CPT17e in HeLa cells is investigated. HeLa cells are cultured with increasing concentrations of CU-CPT17e or poly I:C or blank control (DMSO) for 24 h. Treatment with CU-CPT17e for 24 h at different concentrations (10 to 40 μM) results in an elevation of apoptotic cell population ranging from 10% to 17%, which is more effective than poly I:C at 5 μg/mL. These results suggest that the antiproliferative activity of CU-CPT17e against HeLa cells might result from its ability to directly induce apoptosis[1]. |
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