Bioactivity | C29 is a Toll-like receptor 2 (TLR2) inhibitor. C29 blocks hTLR2/1 and hTLR2/6 signaling with IC50s of 19.7 and 37.6 μM, respectively[1]. | ||||||||||||
Invitro | C29 (10 or 50 μΜ; 1 hour) blocks P3C- and P2C-induced IL-8 mRNA dose-dependently in HEK-TLR2 stable transfectants. C29 (50-200 μM; 1 hour) inhibits P3C- and P2C-induced IL-1β gene expression significantly at both 1 h and 4 h following stimulation in THP-1 cells[1].C29 (25 or 50 μΜ; 1 hour) reduces P3C-induced but not P2C-induced TNF-α mRNA and IL-12 p40 protein significantly in primary murine macrophages[1].C29 (50 μΜ; 1 hour) blocks TLR2 bacterial agonist-induced proinflammatory gene expression in HEK-TLR2 cells and murine macrophages[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
Name | C29 | ||||||||||||
CAS | 363600-92-4 | ||||||||||||
Formula | C16H15NO4 | ||||||||||||
Molar Mass | 285.29 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Mistry P, et al. Inhibition of TLR2 signaling by small molecule inhibitors targeting a pocket within the TLR2 TIR domain. Proc Natl Acad Sci U S A. 2015 Apr 28;112(17):5455-60. [2]. Cai S, Zhu G, Cen X, et al. Synthesis, structure-activity relationships and preliminary mechanism study of N-benzylideneaniline derivatives as potential TLR2 inhibitors. Bioorg Med Chem. 2018;26(8):2041-2050. |