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hTLR7

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By Targets:	HBV (1) IFNAR (1) Interleukin Related (2) NF-κB (1) PD-1/PD-L1 (1) TNF Receptor (1) Toll-like Receptor (TLR) (12)
By Research Areas:	Cancer (5) Infection (1) Inflammation/Immunology (9)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-153460

TLR7/8/9 antagonist 2	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7/8/9 antagonist 2 is an orally active *TLR7/8/9* antagonist. TLR7/8/9 antagonist 2 has inhibitory activities for HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC₅₀ values of 0.011 μM, 0.029 μM and 0,052 μM, respectively.TLR7/8/9 antagonist 2 has high bioavailability in vivo.TLR7/8/9 antagonist 2 can be used for the research of auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis .

HY-144501

D18	Toll-like Receptor (TLR) PD-1/PD-L1	Inflammation/Immunology Cancer
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 (HY-144497). D18 has strong immune activation and anti-tumor activity. D18 commonly used in cancer research, such as colon cancer .

HY-178037

TLR9 antagonist 1	Toll-like Receptor (TLR) Interleukin Related TNF Receptor	Inflammation/Immunology
TLR9 antagonist 1 is a selective *hTLR9* antagonist with an IC₅₀ of 0.1 nM against *hTLR9*. TLR9 antagonist 1 exhibits favorable pharmacokinetic and pharmacodynamic properties. TLR9 antagonist 1 can be used in the research of systemic lupus erythematosus .

HY-159178

m-AM-BBIQ	Toll-like Receptor (TLR)	Inflammation/Immunology
m-AM-BBIQ (compound 10) is a dual *TLR7* and TLR8 agonist, with EC₅₀ values of 0.12 μM and 1.7 μM for hTLR7 and hTLR8, respectively .

HY-153543

TLR7/8 agonist 8	Toll-like Receptor (TLR)	Cancer
TLR7/8 agonist 8 (compound 24m) is a potent toll-like receptor 7/8 (TLR7/8) dual agonist, with EC₅₀s of 27 and 12 nM for *hTLR7* and *hTLR8, respectively. TLR7*/8 agonist 8 can improve the antitumor activity of PD-1/PD-L1 blockade .

HY-170770

TLR7/8 agonist 12	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7/8 agonist 12 (compound 9) is an *hTLR7/8* agonist, with EC₅₀ values of 11 nM (hTLR7) and 150 nM (hTLR8), respectively. TLR7/8 agonist 12 has the potential for immunomodulation .

HY-177300

TLR7/8 agonist 13	Toll-like Receptor (TLR) HBV IFNAR Interleukin Related	Infection Inflammation/Immunology
TLR7/8 agonist 13 is an orally active dual agonist of *TLR7* (lowest effective concentrations (LEC) [hTLR7] = 1.6 μM) and TLR8 (LEC [hTLR8] = 1.6 μM). TLR7/8 agonist 13 exhibits agonistic activity against human peripheral blood mononuclear cells (hPBMCs) (LEC [hPBMC] = 0.5 μM). TLR7/8 agonist 13 induces endogenous IFNα, activating myeloid dendritic cells and monocytes toward a TH1 phenotype in mice and cynomolgus monkeys. TLR7/8 agonist 13 reduces viral load and HBV surface antigen expression in a mouse model of chronic AAV-HBV infection. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, which may promote HBV antigen-specific CD8 T cell-mediated responses. TLR7/8 agonist 13 can be used to study hepatitis B virus .

HY-162115

TLR7 agonist 17	Toll-like Receptor (TLR)	Cancer
TLR7 agonist 17 (compound 20) is a potent *TLR7* agonist with EC₅₀ values of 12 nM and 17 nM for hTLR7 and mTLR7, respectively. TLR7 agonist 17 shows anticancer activity .

HY-162845

TLR7/8 agonist 11	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7/8 agonist 11 (compound 30) is a potent agonist of *hTLR7* and *hTLR8, with EC₅₀s of 31.1 nM and 13.1 nM, respectively. TLR7*/8 agonist 11 plays an important role in adaptive and innate immune responses .

HY-153544

TLR7/8 agonist 9	Toll-like Receptor (TLR)	Cancer
TLR7/8 agonist 9 (Compound 25a) is a *TLR7/8* agonist, with EC₅₀s of 40 nM and 23 nM for hTLR7/8. TLR7/8 agonist 9 has anti-tumor activity and improves the antitumor activity of PD-1/PD-L1 blockade. TLR7/8 agonist 9 can be used for research of cancer immunotherapy .

HY-162116

TLR7 agonist 18	Toll-like Receptor (TLR)	Inflammation/Immunology Cancer
TLR7 agonist 18 (Compound 21a) is a selective Toll-like receptor 7 (TLR7) agonist with an EC₅₀ of 7.8 μM. TLR7 agonist 18 is not cytotoxic to hTLR7 cotransfected HEK293 cell lines and can induce the secretion of several cytokines, including IL-1β, IL-12p70, IL-8, and TNF-α. TLR7 agonist 18 can be used in vaccine, asthma, allergy and anti-cancer research .

HY-183276

TLR8 antagonist-2	Toll-like Receptor (TLR) NF-κB	Inflammation/Immunology
TLR8 antagonist-2 (Compound 35) is a selective TLR8 antagonist with an IC₅₀ of 0.032 μM against hTLR8. TLR8 antagonist-2 potently inhibits TLR8-dependent NF-κB activity in cells stimulated with TL8-506 (HY-20457). TLR8 antagonist-2 can be used in research related to inflammatory and immune diseases .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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hTLR7

Inhibitors & Agonists