1. Immunology/Inflammation NF-κB
  2. Toll-like Receptor (TLR) NF-κB
  3. TLR8 antagonist-2

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.

For research use only. We do not sell to patients.

TLR8 antagonist-2

TLR8 antagonist-2 Chemical Structure

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Description

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[1].

IC50 & Target[1]

hTLR8

0.032 μM (IC50)

In Vitro

TLR8 antagonist-2 (10 μM) potently inhibits TLR8-dependent NF-κB activity in hTLR8-HEK293 reporter cells stimulated by TL8-506, with an IC50 of 0.032 μM[1].
TLR8 antagonist-2 (1 h) potently inhibits TL8-506-induced TNF secretion, with an IC50 value of 0.014 μM in THP-1 macrophages and 0.107 μM in PBMCs[1].
TLR8 antagonist-2 potently inhibits the cellular responses of THP-1 macrophages stimulated by TL8-506, with an IC50 of 0.0022 μM[1].
The half-life of TLR8 antagonist-2 in mouse liver microsomes is 73.6 min[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ELISA Assay[1]

Cell Line: THP-1 macrophages, human peripheral blood mononuclear cells (PBMCs)
Concentration: 0.014 μM (THP-1 TNF IC50); 0.107 μM (PBMC TNF IC50); 1 μM (IL-8 inhibition); up to 50 μM (cytotoxicity test)
Incubation Time: 1 h (preincubation); 4 h (agonist stimulation)
Result: Demonstrated concentration-dependent inhibition of TNF secretion, with an IC50 of 0.014 μM in THP-1 macrophages and 0.107 μM in PBMCs.
Completely inhibited TL8-506-induced IL-8 secretion at 1 μM in both cell types.
Showed no cytotoxicity detected up to 50 μM via LDH assay.
Molecular Weight

418.53

Formula

C25H30N4O2

SMILES

O=C(NC1CCN(C(C)C)CC1)C2=CC=C(COC3=C4C=CC=CC4=NC(C)=N3)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
TLR8 antagonist-2
Cat. No.:
HY-183276
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