TBK1/IKKε-IN-2

TBK1/IKKε-IN-2 is a dual TBK1 and IKKε inhibitor.

Signaling Pathways >> NF-κB >> IKK

Research Areas >> Inflammation/Immunology

TBK1:0.6 nM (IC50, at 5 μM ATP)

IKKε:3.9 nM (IC50, at 10 μM ATP)

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 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].

[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.

Resveratrol | MRT67307 | BMS-345541 | MLN120B | ACHP (Hydrochloride) | TPCA-1 | IKK-16 | IMD 0354 | LY2409881 | SC-514 | BI 605906 | Bay 65-1942 (hydrochloride) | AZD3264 | PS-1145 | IKK-IN-1