产品描述: C29 is a novel inhibitor of TLR2/1 and TLR2/6 signaling induced by synthetic and bacterial TLR2 agonists in human HEK-TLR2 and THP-1 cells, but only TLR2/1 signaling in murine macrophages |
靶点:
TLR |
体外研究:
C29 blunts hTLR2/1 and hTLR2/6 signaling in HEK-TLR2 Stable transfectants and THP-1 Cells. C29 blocks P3C- and P2C-induced IL-8 mRNA dose-dependently in HEK-TLR2 stable transfectants. C29 also inhibits P3C- and P2C-induced IL-1β gene expression significantly at both 1 h and 4 h following stimulation, as well as both P3C- and P2C-induced NF-κB–luciferase activity in transiently transfected HEK293T cells expressing hTLR2 and an NF-κB–sensitive luciferase reporter construct. C29 preferentially inhibits TLR2/1 signaling in primary murine macrophages. C29 blocks TLR2 bacterial agonist-induced proinflammatory gene expression in HEK-TLR2 Cells and murine macrophages. C29 inhibits ligand-induced interaction of TLR2 with MyD88 and blocks MAPK and NF-κB activation |
体内研究:
C29L inhibits TLR2/1-induced inflammation in mice. Mice treated twice with C29L before administration of P3C significantly blocks IL-12 p40 and TNF-α liver cytokine mRNA and serum protein. C29L has a significant inhibitory effect at the later time point for IL-12 p40 |
参考文献:
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. Du J, Li J, Zhu J, et al. Structural characterization and immunomodulatory activity of a novel polysaccharide from Ficus carica[J]. Food & function. 2018 Jul 17;9(7):3930-3943. 3. Li Y, Niu M, Zhao A, et al. CXCL12 is involved in α-synuclein-triggered neuroinflammation of Parkinson’s disease[J]. Journal of Neuroinflammation. 2019, 16(1): 1-14. 4. Jiang S, Yin H, Qi X, et al. Immunomodulatory effects of fucosylated chondroitin sulfate from Stichopus chloronotus on RAW 264.7 cells[J]. Carbohydrate Polymer. 2020, 251: 117088. 5. Wen Y, Peng D, Li C, et al. A new polysaccharide isolated from Morchella importuna fruiting bodies and its immunoregulatory mechanism[J]. International Journal of Biological Macromolecules. 2019, 137: 8-19. |
溶解性:
Soluble in DMSO |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
3.505 ml |
17.526 ml |
35.051 ml |
5 mM |
0.701 ml |
3.505 ml |
7.01 ml |
10 mM |
0.351 ml |
1.753 ml |
3.505 ml |
50 mM |
0.07 ml |
0.351 ml |
0.701 ml |
|
注意: |
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