Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
1.9219 mL
9.6093 mL
19.2186 mL
5 mM
0.3844 mL
1.9219 mL
3.8437 mL
10 mM
0.1922 mL
0.9609 mL
1.9219 mL
50 mM
0.0384 mL
0.1922 mL
0.3844 mL
Description
GSK8612 is a highly potent and selective inhibitor for with pKd of 8.0. Within 10-fold affinity with respect to TBK1, no off-targets of GSK8612 could be identified.
In cellular assays, this small molecule inhibits toll-like receptor (TLR)3-induced interferon regulatory factor (IRF)3 phosphorylation in Ramos cells and type I interferon (IFN) secretion in primary human mononuclear cells. In THP1 cells, GSK8612 is able to inhibit secretion of interferon beta (IFNβ) in response to dsDNA and cGAMP, the natural ligand for STING. GSK8612 has lower affinity for phosphorylated TBK1. GSK8612 inhibits recombinant TBK1 with an average pIC50 of 6.8 in a biochemical functional assay. The actual selectivity of GSK8612 for TBK1 in the cells will depend on the activation state of TBK1.
