TH023

TH023 is an inhibitor for the TLR4 signaling pathway, that targets especially the formation of TLR4 homodimer. TH023 inhibits secreted embryonic alkaline phosphatase in cell HEK-Blue hTLR4 with an IC50 of 0.354 μM, and inhibits the NO expression in RAW264.7 with an IC50 of 1.61μM. TH023 also inhibits the activation of NF-κB, reduces the nuclear translocation of NF-κB p65. TH023 exhibits anti-inflammatory efficacy in LPS (HY-D1056) -induced mouse acute sepsis model, and ameliorates the mouse lung injury[1].

Product Specifications

UNSPSC

12352005

Target

NF-κB; Toll-like Receptor (TLR)

Type

Reference compound

Related Pathways

Immunology/Inflammation; NF-κB

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/th023.html

Smiles

O=C(C1=C2N=C(C3=CC=C(Cl)C=C3)C=C(C(F)F)N2N=C1)N4C[C@]5([H])CCCC[C@]5([H])C4

Molecular Formula

C22H21ClF2N4O

Molecular Weight

430.88

References & Citations

[1]Jiang YY, et al., Discovery of pyrazolo[1,5-a]pyrimidine derivatives targeting TLR4-TLR4∗ homodimerization via AI-powered next-generation screening. Eur J Med Chem. 2024 Oct 6;280:116945.