An inhibitor of the TLR5-flagellin protein-protein interaction
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TH1020

Item No. 33553

Technical Information
Formal Name
4-[[4-(phenylmethyl)-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]thio]-pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine
CAS Number
1841460-82-9
Molecular Formula
C23H15N7S2
Formula Weight
Purity
≥98%
A crystalline solid
Chloroform: 1 mg/ml
λmax
236, 267, 293 nm
SMILES
C1(C2=CC=NC=C2)=NN=C(SC3=C4C(C5=CC=CN=C5S4)=NC=N3)N1CC6=CC=CC=C6
InChi Code
InChI=1S/C23H15N7S2/c1-2-5-15(6-3-1)13-30-20(16-8-11-24-12-9-16)28-29-23(30)32-22-19-18(26-14-27-22)17-7-4-10-25-21(17)31-19/h1-12,14H,13H2
InChi Key
CBBXTGWSGPEJEE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    TH1020 is an inhibitor of the protein-protein interaction between toll-like receptor 5 (TLR5) and flagellin.1 It binds to the TLR5 heterodimer interface to disrupt TLR5-flagellin tetramer formation and inhibits flagellin-induced TLR5 signaling in TLR5-overexpressing HEK cells (IC50 = 0.85 µM). TH1020 (0.37 µM) inhibits flagellin-induced, TLR5-mediated secretion of TNF-α in primary human peripheral blood mononuclear cells (PBMCs).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yan, L., Liang, J., Yao, C., et alPyrimidine triazole thioether derivatives as toll-like receptor 5 (TLR5)/flagellin complex inhibitors. ChemMedChem 11(8), 822-826 (2016).