Molecular Formula | C26H36N6O2 |
Molar Mass | 464.6 |
Density | 1.270 |
Solubility | H2O: soluble15mg/mL, clear |
Appearance | powder |
Color | white to light brown |
pKa | 15.94±0.20(Predicted) |
Storage Condition | Keep in dark place,Sealed in dry,2-8°C |
In vitro study | In macrophages, MRT67307 prevented IRF3 phosphorylation and IFNβ production. In wild-type MEF cells, MRT67307 enhanced the Ser933 phosphorylation of p105 stimulated by IL-1 and the phosphorylation of Ser468 and Ser536 of RelA, and IL-1 stimulated NF-Δb-dependent gene transcriptional activation was enhanced. In addition, the promotion of IL-10 production by MRT67307 and the inhibition of pro-inflammatory cytokines are achieved through a crtc3-dependent pattern. MRT67307 also inhibited ULK in MEF cells and blocked autophagy. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.152 ml | 10.762 ml | 21.524 ml |
5 mM | 0.43 ml | 2.152 ml | 4.305 ml |
10 mM | 0.215 ml | 1.076 ml | 2.152 ml |
5 mM | 0.043 ml | 0.215 ml | 0.43 ml |
biological activity | MRT67307 is a highly effective dual IKK/TBK1 inhibitor with IC50 of 160 and 19 nM respectively. MRT67307 can effectively inhibit ULK1 and ULK2 and restrict autophagy. |
target | TargetValue IKK (Cell-Free Assay) 160 nM TBK1 (Cell-Free Assay) 190 nM |
Target | Value |
IKKϵ (Cell-free assay) | 160 nM |
TBK1 (Cell-free assay) | 190 nM |
In vitro study | In macrophages, MRT67307 prevented IRF3 phosphorylation and IFNβ production. In wild-type MEF cells, MRT67307 enhanced IL-1-stimulated Ser933 phosphorylation of p105 and Ser468 and Ser536 phosphorylation of RelA, and enhanced IL-1-stimulated NF-κB-dependent gene transcriptional activation. In addition, MRT67307 promotion of IL-10 production and inhibition of pro-inflammatory cytokines are achieved through CRTC3-dependent patterns. MRT67307 also inhibited ULK in MEF cells and blocked autophagy. |