GSK8612 Struktur

GSK8612

Bezeichnung:GSK8612

CAS-Nr2361659-62-1

Englisch Name:GSK8612

CBNumberCB95489258

SummenformelC17H17BrF3N7O2S

Molgewicht520.33

MOL-Datei2361659-62-1.mol

GSK8612 physikalisch-chemischer Eigenschaften

Siedepunkt	671.0±65.0 °C(Predicted)
Dichte	1.74±0.1 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	Soluble in DMSO (20 mg/ml)
pka	10.07±0.10(Predicted)
Aggregatzustand	solid
Farbe	Beige
Stabilität	Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

Gefahreninformationscode (GHS)

GSK8612 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
GSK8612 (2361659-62-1) is a highly selective and potent (avg. pIC50 = 6.8 versus recombinant TBK1) inhibitor of Tank-binding Kinase-1 (TBK1) with higher affinity for unactivated TBK1.? It inhibited phosphorylation of IRF3 (pIC50 = 6.0), inhibited the release of IFNa from human PBMC’s (pIC50 = 6.1), and inhibited IFNb secretion from THP-1 cells (pIC50 = 5.8 dsDNA virus, 6.3 cGAMP stilmulated cells).
Verwenden
GSK 8612 is a highly selective TBK1 Inhibitor involved in regulating signaling pathways in immune responses.
Biologische Aktivität
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.
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.
Einzelnachweise
Thomson et al. (2019), Discovery of a GSK8612, a Highly Selective and Potent TBK1 Inhibitor; ACS Med. Chem. Lett., 10 780

GSK8612 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

2361659-62-1, GSK8612 Verwandte Suche:

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