Name | TBK1/IKKε-IN-5 |
Synonyms | Benzonitrile, 5-[4-[[4-[4-(3-oxetanyl)-1-piperazinyl]phenyl]amino]-1,3,5-triazin-2-yl]-2-[(tetrahydro-2H-pyran-4-yl)oxy]- |
CAS | 1893397-65-3 |
Molecular Formula | C28H31N7O3 |
Molar Mass | 513.59 |
Solubility | DMSO : 7.81 mg/mL (15.21 mM; Need ultrasonic) |
Storage Condition | -20°C |
Use | TBK1/IKKε-IN-5 (compound 1) is a double inhibitor of TBK1 and IKKε, and its IC50 values are 1 nM and 5.6 nM, respectively. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.947 ml | 9.735 ml | 19.471 ml |
5 mM | 0.389 ml | 1.947 ml | 3.894 ml |
10 mM | 0.195 ml | 0.974 ml | 1.947 ml |
5 mM | 0.039 ml | 0.195 ml | 0.389 ml |
biological activity | TBK1/ikkδ-in-5 (compound 1) is a TANK-binding kinase 1 (TBK1) the IC50 values for dual inhibitors of and IκB kinase-ε (IKK ε/IKK-i) are 1.0 nM and 5.6 nM for TBK1 and IKK ε, respectively. Inhibition of TBK1 /IKK ε enhances the response to PD-1 blockade, effectively predicting tumor response in vivo. |
Target | Value |
TBK1 (Cell-free assay) | 1.0 nM |
IKKε (Cell-free assay) | 5.6 nM |