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TBK1/IKKε-IN-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TBK1/IKKε-IN-1图片
CAS NO:1292310-49-6
规格:≥98%
包装与价格:
包装价格(元)
5mg询价
10mg询价
25mg询价
50mg询价
100mg询价

理化性质和储存条件


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 InformationSynonym: 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
实验参考方法
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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