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经验公式(希尔记法):
C17H17BrF3N7O2S
化学文摘社编号:
分子量:
520.33
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
FC(F)(F)C[n]1nc(c(c1)Nc2nc(c(cn2)Br)NCc3ccc(cc3)[S](=O)(=O)N)C
InChI key
FFPHMUIGESPOTK-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
GSK8612 is a potent and highly selective tank-binding kinase-1 (TBK1) inhibitor (pIC50 = 6.8; pKd = 8.0 vs pKa = 6.2/STK17B, 6.0/IKKε, 6.1/LRRK2, 6.0/FLT4, 5.8/ULK3, 5.7/BMP2K, 5.7/CSNK2A1, 5.6/CSNK2A2, 5.6/FLT4, 5.5/PIK3CD, <5.5/more than 270 kinases). GSK8612 inhibits IFNβ secretion induced by dsDNA containing virus or STING ligand cGAMP (IC50 = 1.25 & 0.5 μM, respectively; THP-1), as well as suppresses TLR3 ligand poly(I:C)-induced IRF3 Ser396 phosphorylation (IC50 = 1 μM; Ramos) and IFNα release (IC50 = 0.79 μM; human PBMCs), a IFN positive feedback response steming from IFNβ.
Potent and highly selective tank-binding kinase-1 (TBK1) inhibitor.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Douglas W Thomson et al.
ACS medicinal chemistry letters, 10(5), 780-785 (2019-05-18)
The serine/threonine protein kinase TBK1 (Tank-binding Kinase-1) is a noncanonical member of the IkB kinase (IKK) family. This kinase regulates signaling pathways in innate immunity, oncogenesis, energy homeostasis, autophagy, and neuroinflammation. Herein, we report the discovery and characterization of a
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