1292310-49-6

1292310-49-6 structure

Name: TBK1/IKKε-IN-2
Chemical Name: 5-(2-((4-Morpholinophenyl)Amino)Pyrimidin-4-Yl)-2-((Tetrahydro-2H-Pyran-4-Yl)Oxy)Benzonitrile
CAS Number: 1292310-49-6
Molecular Formula: C₂₆H₂₇N₅O₃
Molecular Weight: 457.524
Catalog: Signaling Pathways NF-κB IKK
Create Date: 2018-02-21 00:24:48
Modify Date: 2024-01-04 10:57:29
TBK1/IKKε-IN-2 is a dual TBK1 and IKKε inhibitor.

Name	5-(2-((4-Morpholinophenyl)Amino)Pyrimidin-4-Yl)-2-((Tetrahydro-2H-Pyran-4-Yl)Oxy)Benzonitrile
Synonyms	5-(2-{[4-(4-Morpholinyl)phenyl]amino}-4-pyrimidinyl)-2-(tetrahydro-2H-pyran-4-yloxy)benzonitrile Benzonitrile, 5-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-2-[(tetrahydro-2H-pyran-4-yl)oxy]- IKK epsilon-IN-1 IKKε-IN-1 TBK1/IKKε-IN-2

Description	TBK1/IKKε-IN-2 is a dual TBK1 and IKKε inhibitor.
Related Catalog	Signaling Pathways >> NF-κB >> IKK Research Areas >> Inflammation/Immunology
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.