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TLR ligands

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By Targets:	Toll-like Receptor (TLR) (17) Amyloid-β (1) Apoptosis (1) ATM/ATR (1) IFNAR (1) Interleukin Related (2) Phosphatase (1) Pyroptosis (1)
By Research Areas:	Cancer (4) Infection (2) Inflammation/Immunology (16) Neurological Disease (1)

19

Inhibitors & Agonists

1

Screening Libraries

2

Peptides

Targets Recommended: Toll-like Receptor (TLR) Ligands for Target Protein for PROTAC Ligands for E3 Ligase Target Protein Ligand-Linker Conjugates E3 Ligase Ligand-Linker Conjugates

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

Enpatoran 3 Publications Verification M5049	Toll-like Receptor (TLR)	Inflammation/Immunology
Enpatoran (M5049) is a potent, orally active and dual *TLR7/8* inhibitor with IC₅₀s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .

Enpatoran hydrochloride 3 Publications Verification M5049 hydrochloride	Toll-like Receptor (TLR)	Inflammation/Immunology
Enpatoran (M5049) hydrochloride is a potent, orally active and dual *TLR7/8* inhibitor with IC₅₀s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research .

ECDD-S16	Pyroptosis	Inflammation/Immunology
ECDD-S16 is a potent inhibitor of pyroptosis. ECDD-S16 inhibits surface and endosomal TLR ligands activated pyroptosis in Raw264.7 cells .

Pam2CSK4	Toll-like Receptor (TLR)	Inflammation/Immunology
Pam2CSK4, a lipopeptide, is a TLR6-independent *TLR2* ligand and agonist. Pam2CSK4 promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 also activates iNOS expression and NO production in mouse macrophages .

Pam2CSK4 TFA	Toll-like Receptor (TLR)	Inflammation/Immunology
Pam2CSK4 (TFA), a lipopeptide, is a TLR6-independent *TLR2* ligand and agonist. Pam2CSK4 (TFA) promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 (TFA) also activates iNOS expression and NO production in mouse macrophages .

Polyinosinic acid	Toll-like Receptor (TLR)	Inflammation/Immunology
Polyinosinic acid is a single stranded homonucleic acid, which is a Toll-like Receptor 3 (TLR3) ligand. Polyinosinic acid enhances cellular immune response through TLR3 and TRIF. Polyinosinic acid has potential applications in immune regulation .

AXC-715 hydrochloride T785 hydrochloride	Toll-like Receptor (TLR)	Inflammation/Immunology
AXC-715 (T785) hydrochloride is a *TLR7/TLR8* dual agonist, extracted from patent WO2020168017 A1 . AXC-715, 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 .

AXC-715 trihydrochloride T785 trihydrochloride	Toll-like Receptor (TLR)	Inflammation/Immunology
AXC-715 (T785) 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 .

Polyinosinic acid sodium	Toll-like Receptor (TLR)	Inflammation/Immunology
Polyinosinic acid sodium is the sodium form of Polyinosinic acid (HY-148980). Polyinosinic acid is a single stranded homonucleic acid, which is a Toll-like Receptor 3 (TLR3) ligand. Polyinosinic acid enhances cellular immune response through TLR3 and TRIF. Polyinosinic acid has potential applications in immune regulation .

TMX-201	Toll-like Receptor (TLR)	Cancer
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 .

Biotin-labeled ODN 2216 sodium	Toll-like Receptor (TLR)	Inflammation/Immunology
Biotin-labeled ODN 2216 (sodium) is a human-specific *TLR9* (toll-like receptor 9) ligand or agonist. Biotin-labeled ODN 2216 (sodium) can be used to evaluate CpG ODN cellular uptake and localization using a biotin detection system and light microscopy.

ODN 2007	Toll-like Receptor (TLR)	Infection Inflammation/Immunology
ODN 2007, a class B CpG ODN (oligodeoxynucleotide), is a Toll-like receptor (TLR) ligand. ODN 2007 can be used as an immunomodulator, vaccine adjuvant, and enhance immune responses in mammals, fish, and humans. ODN 2007 sequence: 5'-TCGTCGTTGTCGTTTTGTCGTT-3' .

FITC-labeled ODN 2216 sodium	Toll-like Receptor (TLR) Interleukin Related	Inflammation/Immunology
FITC-labeled ODN 2216 (sodium) is a human-specific *TLR9* (toll-like receptor 9) ligand or agonist. FITC-labeled ODN 2216 (sodium) can be used to evaluate CpG ODN cellular uptake and localization by confocal laser-scanning microscopy (excitation 495 nm, emission 520 nm) or flow cytometry.

ODN INH 18	Toll-like Receptor (TLR)	Inflammation/Immunology
ODN INH-18 is a linear 24-mer class B INH-ODN in which the 5' INH-ODN 4084-F sequence was followed by a random stretch of 12 nucleotides lacking the ability to form significant secondary structures. ODN INH-18 showes inhibitory potency for TLR9 ligand-induced IFN-α production.

ODN INH 18 sodium	Toll-like Receptor (TLR)	Inflammation/Immunology
ODN INH-18 sodium is a linear 24-mer class B INH-ODN in which the 5' INH-ODN 4084-F sequence was followed by a random stretch of 12 nucleotides lacking the ability to form significant secondary structures. ODN INH-18 sodium showes inhibitory potency for TLR9 ligand-induced IFN-α production.

ODN 2216 1 Publications Verification	Toll-like Receptor (TLR) IFNAR Interleukin Related	Infection Inflammation/Immunology Cancer
ODN 2216 is a human-specific *TLR9* (toll-like receptor 9) ligand or agonist. ODN 2216 induces high amounts of IFN-α and IFN-β. ODN 2216 induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 can activate NK cells and promote IFN-γ production of TCR-triggered CD4 ⁺ T cells .

ODN 2216 sodium	Toll-like Receptor (TLR)	Cancer
ODN?2216 sodium is a human-specific *TLR9* (toll-like receptor 9) ligand or agonist. ODN?2216 sodium induces high amounts of IFN-α and IFN-β. ODN 2216 sodium induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 sodium stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 sodium can activate NK cells and promote IFN-γ production of TCR-triggered CD4 ⁺ T cells .

Ro 90-7501 1 Publications Verification	Amyloid-β ATM/ATR Phosphatase Apoptosis	Neurological Disease Cancer
Ro 90-7501 is an amyloid β₄₂ (Aβ₄₂) fibril assembly inhibitor that reduces Aβ₄₂-induced cytotoxicity (EC₅₀ of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response . Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner . Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells .

Complete Freund's adjuvant (CFA)	Toll-like Receptor (TLR)	Inflammation/Immunology
Complete Freund's adjuvant (CFA) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund to enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA) stimulates a strong and durable immune response and can be used to induce persistent inflammatory pain models in mice, experimental autoimmune myocarditis (EAM) models, and more. Incomplete Freund's adjuvant (IFA) (HY-153808A) is another type of Freund's Adjuvant that stimulates a weaker immune response .

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