A thiophenecarboxamidopropionate compound that acts as a direct, competitive and high affinity inhibitor of dsRNA binding to TLR3 (Ki = 2.96 µM; Kd = 19 nM for dsRNA binding to TLR3) and selectively antagonizes stimulated TLR3 signaling without affecting TLR1/2, TLR2/6, TLR4 and TLR7 pathways. Shown to efficiently repress TNF-α and IL-1β (IC90 = 27 µM) and NO production (IC50 = 3.44 µM) in Poly(I:C)-induced RAW 264.7 macrophages. Exhibits minimal cytotoxicity (IC50 >>100 µM in RAW 264.7 cells) and is weakly active against a panel of 12-representative kinases and 4-cytochrome enzymes (in vitro assays).
Other Notes
Cheng, K., et al. 2011. J. Am. Chem. Soc.133, 3764.
Packaging
Packaged under inert gas
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
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