TLR4-IN-2 (Compound Racemic-11k) is inhibitors of TLR4, JNK, and NF-kappaB. TLR4-IN-2 inhibits NO production in LPS-stimulated RAW264.7 cells with an IC50 value of 23.2 µM. TLR4-IN-2 exerts anti-inflammatory activity by inhibiting TLR4 expression, reducing JNK phosphorylation, thereby suppressing the activation of NF-kappaB, blocking the transcription of inflammation-related genes, reducing the expression of iNOS and COX-2, and decreasing the production of inflammatory mediators such as NO, PGE 2, and TNF-alpha. TLR4-IN-2 is promising for research of inflammatory diseases, such as rheumatoid arthritis and various inflammatory disorders[1].
