| CAS NO: | 1292310-49-6 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Name: TBK1/IKKε-IN-1 Molecular Weight: 457.52 Formula: C26H27N5O3 CAS No.: 1292310-49-6 SMILES: N#CC1=CC(C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2)=CC=C1OC5CCOCC5 | |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Technical Information | Synonym: IKK epsilon-IN-1; IKKεIN-2; IKKε-IN-1; IKKε IN-1; IKKεIN2; IKKεIN 1; IKKε-IN-2 Chemical Name: 5-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)-2-((tetrahydro-2H-pyran-4-yl)oxy)benzonitrile InChi Key: BWABTWGSXHTHCG-UHFFFAOYSA-N InChi Code: InChI=1S/C26H27N5O3/c27-18-20-17-19(1-6-25(20)34-23-8-13-32-14-9-23)24-7-10-28-26(30-24)29-21-2-4-22(5-3-21)31-11-15-33-16-12-31/h1-7,10,17,23H,8-9,11-16H2,(H,28,29,30) SMILES Code: N#CC1=CC(C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2)=CC=C1OC5CCOCC5 |
| Target |
TBK1:0.6 nM (IC50, at 5 μM ATP) IKKε:3.9 nM (IC50, at 10 μM ATP) |
|---|---|
| In Vitro | TBK1/IKKε-IN-2 (Cmpound #1) inhibits TBK1 biochemical function in Ulight kinase assay at 5 and 250 μM ATP concentration with IC50s of 0.6 and 2.6 nM, rsespectively. TBK1/IKKε-IN-2 inhibits IKKε biochemical function in Ulight kinase assay at 10 μM ATP with an IC50 of 3.9 nM. The IC50 of TBK1/IKKε-IN-2 in the Panc 02.13 proliferation assay is 5 μM[1]. |
| Cell Assay | Cell proliferation experiments are carried out in a 96-well format (6 replicates), Panc 02.13 cells are plated at a density of 2,000 to 5,000 cells per well. At 24 hours following cell seeding, the cells are treated with the tool inhibitor titrations (e.g., TBK1/IKKε-IN-2, 1 nM, 10 nM, 100 nM, 1 μM and 10 μM) for 4 days at 37°C and then assayed by using the ATP CellTiter-Glo luminescent cell viability assay[1]. |
| References |
[1]. Muvaffak A, et al. Evaluating TBK1 as a therapeutic target in cancers with activated IRF3. Mol Cancer Res. 2014 Jul;12(7):1055-66 |
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