GSK8612
- Product Name
- GSK8612
- CAS No.
- 2361659-62-1
- Chemical Name
- GSK8612
- Synonyms
- GSK8612;GSK8612;GSK-8612;GSK 8612;Inhibitor,IKK,I kappa B kinase,GSK 8612,GSK-8612,GSK8612,inhibit,IκB kinase;4-(((5-Bromo-2-((3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)amino)methyl)benzenesulfonamide;Benzenesulfonamide, 4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]amino]-4-pyrimidinyl]amino]methyl]-
- CBNumber
- CB95489258
- Molecular Formula
- C17H17BrF3N7O2S
- Formula Weight
- 520.33
- MOL File
- 2361659-62-1.mol
GSK8612 Property
- Boiling point:
- 671.0±65.0 °C(Predicted)
- Density
- 1.74±0.1 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- Soluble in DMSO (20 mg/ml)
- form
- solid
- pka
- 10.07±0.10(Predicted)
- color
- Beige
- Stability:
- Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0094203
- Product name
- GSK8612
- Purity
- 98.79%
- Packaging
- 25mg
- Price
- $590
- Updated
- 2021/12/16
- Product number
- CS-0094203
- Product name
- GSK8612
- Purity
- 98.79%
- Packaging
- 5mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- CS-0094203
- Product name
- GSK8612
- Purity
- 98.79%
- Packaging
- 10mg
- Price
- $280
- Updated
- 2021/12/16
- Product number
- Axon3007
- Product name
- GSK8612
- Purity
- 99%
- Packaging
- 5mg
- Price
- $132
- Updated
- 2021/12/16
- Product number
- CS-0094203
- Product name
- GSK8612
- Purity
- 98.79%
- Packaging
- 50mg
- Price
- $950
- Updated
- 2021/12/16
GSK8612 Chemical Properties,Usage,Production
Description
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).
Uses
GSK 8612 is a highly selective TBK1 Inhibitor involved in regulating signaling pathways in immune responses.
Biological Activity
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.
References
Thomson et al. (2019), Discovery of a GSK8612, a Highly Selective and Potent TBK1 Inhibitor; ACS Med. Chem. Lett., 10 780
GSK8612 Preparation Products And Raw materials
Raw materials
Preparation Products
GSK8612 Suppliers
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