| Description | 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. |
| In vitro | 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[1]. |
| In vivo | 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[1]. |
| molecular weight | 285.29 |
| Molecular formula | C16H15NO4 |
| CAS | 363600-92-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: Insoluble DMSO: 60 mg/mL (210.3 mM) |
| References | 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. 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. 4. 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. 5. 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. |
| Citations | 1. Jiang S, Yin H, Qi X, et al. Immunomodulatory effects of fucosylated chondroitin sulfate from Stichopus chloronotus on RAW 264.7 cells. Carbohydrate Polymer. 2020, 251: 117088. 2. Nie K, Zhang C, Deng M, et al. A Series of Genes for Predicting Responses to Anti-Tumor Necrosis Factor α Therapy in Crohn’s Disease. Frontiers in Pharmacology. 2022: 1195 3. Li Y, Niu M, Zhao A, et al. CXCL12 is involved in α-synuclein-triggered neuroinflammation of Parkinson’s disease. Journal of Neuroinflammation. 2019, 16(1): 1-14 4. Wen Y, Peng D, Li C, et al. A new polysaccharide isolated from Morchella importuna fruiting bodies and its immunoregulatory mechanism. International Journal of Biological Macromolecules. 2019, 137: 8-19. 5. Du J, Li J, Zhu J, et al. Structural characterization and immunomodulatory activity of a novel polysaccharide from Ficus carica. Food & function. 2018 Jul 17;9(7):3930-3943. 6. Zhang R, Tang L, Wang Y, et al.A Dendrimer Peptide (KK2DP7) Delivery System with Dual Functions of Lymph Node Targeting and Immune Adjuvants as a General Strategy for Cancer Immunotherapy.Advanced Science.2023: 2300116. |