Molecular Formula | C16H15NO4 |
Molar Mass | 285.29 |
Density | 1.21±0.1 g/cm3(Predicted) |
Melting Point | >192°C (dec.) |
Boling Point | 505.7±50.0 °C(Predicted) |
Solubility | DMSO: ≥ 30 mg/mL |
Appearance | Solid |
Color | Dark Orange |
pKa | 4.01±0.10(Predicted) |
Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
Stability | Moisture Sensitive |
In vitro study | 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. 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. C29 (50 μΜ; 1 hour) blocks TLR2 bacterial agonist-induced proinflammatory gene expression in HEK-TLR2 cells and murine macrophages. Western Blot Analysis Cell Line: THP-1 cells Concentration: 150 μM Incubation Time: 1 hours Result: Diminished the interaction between endogenous TLR2 and myeloid differentiation primary response gene 88 (MyD88) at 15 and 30 min poststimulation with P3C. Western Blot Analysis Cell Line: Murine peritoneal macrophages Concentration: 50 μM Incubation Time: 1 hours Result: Blocked robust MAPK activation at 30 min and reduced NF-κB activation from 5 to 30 min. Prevented P3C-induced degradation of IκBα at 15 and 30 min. |
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 |
5 mM | 0.07 ml | 0.351 ml | 0.701 ml |
biological activity | TLR2-IN-C29 (C29) is an inhibitor of Toll-like receptor 2 (TLR2), which can inhibit TLR2/1 and TLR2/6 Signal transduction. |
target | TargetValue TLR2 () |
Target | Value |
in vitro study | C29 (10 or 50 μM; 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. C29 (25 or 50 μM; 1 hour) reduces P3C-induced but not P2C-induced TNF-α mRNA and IL-12 p40 protein significantly in primary murine macrophages. C29 (50 μM); 1 hour) blocks TLR2 bacterial agonist-induced proinflammatory gene expression in HEK-TLR2 cells and murine macrophages. Western Blot Analysis Cell Line: THP-1 cells Concentration: 150 μM Incubation Time: 1 hours Result: Diminished the interaction between endogenous TLR2 and myeloid differentiation primary response gene 88 (MyD88) at 15 and 30 min poststimulation with P3C. Western Blot Analysis Cell Line: Murine peritoneal macrophages Concentration: 50 μM Incubation Time: 1 hours Result: Blocked robust MAPK activation at 30 min and reduced NF-κB activation from 5 to 30 min. Prevented P3C-induced degradation of IκBα at 15 and 30 min. |
Cell Line: | THP-1 cells Murine peritoneal macrophages |
Concentration: | 150 μM 50 μM |
Incubation Time: | 1 hours 1 hours |
Result: | Diminished the interaction between endogenous TLR2 and myeloid differentiation primary response gene 88 (MyD88) at 15 and 30 min poststimulation with P3C. Blocked robust MAPK activation at 30 min and reduced NF-κB activation from 5 to 30 min. Prevented P3C-induced degradation of IκBα at 15 and 30 min. |