GSK8612 - 98%, high purity , CAS No.2361659-62-1, Inhibitor of inhibitor of nuclear factor kappa B kinase subunit epsilon;Inhibitor of TANK binding kinase 1
GSK8612 - 98%, high purity , CAS No.2361659-62-1, Inhibitor of inhibitor of nuclear factor kappa B kinase subunit epsilon;Inhibitor of TANK binding kinase 1
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.
Storage Temp
Protected from light,Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of inhibitor of nuclear factor kappa B kinase subunit epsilon;Inhibitor of TANK binding kinase 1
Product Description
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.
1.Tanaka Y, Chen ZJ. (2012) STING specifies IRF3 phosphorylation by TBK1 in the cytosolic DNA signaling pathway.. Sci Signal, 5 (214):(ra20). [PMID:22394562]
2.Zhan Z, Cao H, Xie X, Yang L, Zhang P, Chen Y, Fan H, Liu Z, Liu X. (2015) Phosphatase PP4 Negatively Regulates Type I IFN Production and Antiviral Innate Immunity by Dephosphorylating and Deactivating TBK1.. J Immunol, 195 (8):(3849-57). [PMID:26363053]
3.Thomson DW, Poeckel D, Zinn N, Rau C, Strohmer K, Wagner AJ, Graves AP, Perrin J, Bantscheff M, Duempelfeld B et al.. (2019) Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor.. ACS Med Chem Lett, 10 (5):(780-785). [PMID:31097999]
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