GSK8612是高效选择性TBK1抑制剂，pKd为8。 Information GSK8612 GSK8612 is a highly potent and selective inhibitor for TBK1 (Tank-binding Kinase-1) with pKd of 8.0. Within 10-fold affinity with respect to TBK1, no off-targets of GSK8612 could be identified. Targets TBK1 6.8(pIC50) In vitro 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. In vivo GSK8612 is highly protein bound in mouse, rat and human blood.
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GSK8612
CAS number：2361659-62-1 molecular formula：C17H17BrF3N7O2S
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| Chinese alias | - | ||
| English alias | Benzenesulfonamide,4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]amino]-4-pyrimidinyl]amino]methyl]- | ||
| CAS number | 2361659-62-1 | molecular formula | C17H17BrF3N7O2S |
| molecular weight | 520.33 g/mol | Exact mass | - |
| PSA | 136.000 Ų | logp | 3.447 |
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