GSK8612

ChemicalBook > CAS DataBase List > 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;4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]amino]-4-pyrimidinyl]amino]methyl]-benzenesulfonamide;Benzenesulfonamide, 4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]amino]-4-pyrimidinyl]amino]methyl]-;4-(((5-Bromo-2-((3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)amino)methyl)benzenesulfonamide , GSK8612
CBNumber: CB95489258
Molecular Formula: C17H17BrF3N7O2S
Formula Weight: 520.33
MOL File: 2361659-62-1.mol

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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.

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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.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0094203
Product name: GSK8612
Purity: 98.79%
Packaging: 25mg
Price: $590
Updated: 2021/12/16

ChemScene

Product number: CS-0094203
Product name: GSK8612
Purity: 98.79%
Packaging: 5mg
Price: $180
Updated: 2021/12/16

ChemScene

Product number: CS-0094203
Product name: GSK8612
Purity: 98.79%
Packaging: 10mg
Price: $280
Updated: 2021/12/16

Axon Medchem

Product number: Axon3007
Product name: GSK8612
Purity: 99%
Packaging: 5mg
Price: $132
Updated: 2021/12/16

ChemScene

Product number: CS-0094203
Product name: GSK8612
Purity: 98.79%
Packaging: 50mg
Price: $950
Updated: 2021/12/16

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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

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2361659-62-1, GSK8612Related Search:

Tigecycline 9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one METHOPRENE ACID Imiquimod 4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol 1-(1-(3-methoxyphenyl)-7-propoxyindolizin-3-yl)ethanone GSK8612 GSK6853 2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoicacid GSK620 GSK591 GSK5959 ROR gamma-t-IN-1 GSK872 Cadmium sulfide

Benzenesulfonamide, 4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]amino]-4-pyrimidinyl]amino]methyl]-

GSK8612;GSK-8612;GSK 8612

GSK8612

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

4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]amino]-4-pyrimidinyl]amino]methyl]-benzenesulfonamide

4-(((5-Bromo-2-((3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)amino)methyl)benzenesulfonamide , GSK8612

2361659-62-1

C17H17BrF3N7O2S