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GSK8612

GSK8612 structure

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]-

CBNumber:: CB95489258

Molecular Formula:: C17H17BrF3N7O2S

Molecular Weight:: 520.33

MDL Number:: MFCD32062739

MOL File:: 2361659-62-1.mol

Last updated:2023-09-20 16:43:00

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GSK8612 Properties

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)
pka	10.07±0.10(Predicted)
form	solid
color	Beige
Stability	Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

SAFETY

Risk and Safety Statements

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319-H335
Precautionary statements	P261-P305+P351+P338

GSK8612 price

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
ChemScene	CS-0094203	GSK8612 98.79%	2361659-62-1	25mg	$590	2021-12-16	Buy
ChemScene	CS-0094203	GSK8612 98.79%	2361659-62-1	5mg	$180	2021-12-16	Buy
ChemScene	CS-0094203	GSK8612 98.79%	2361659-62-1	10mg	$280	2021-12-16	Buy
Axon Medchem	Axon3007	GSK8612 99%	2361659-62-1	5mg	$132	2021-12-16	Buy
ChemScene	CS-0094203	GSK8612 98.79%	2361659-62-1	50mg	$950	2021-12-16	Buy

Product number	Packaging	Price	Buy
CS-0094203	25mg	$590	Buy
CS-0094203	5mg	$180	Buy
CS-0094203	10mg	$280	Buy
Axon3007	5mg	$132	Buy
CS-0094203	50mg	$950	Buy

GSK8612 Chemical Properties,Uses,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

Global( 45)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32760	60
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10522	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58
Nanjing Doge Biomedical Technology Co., Ltd	+86-25-58227606 +86-15305155328	sales@dogechemical.com	China	4128	58
TargetMol Chemicals Inc.	+1-781-999-5354	support@targetmol.com	United States	19973	58
Wuhan Topule Biopharmaceutical Co., Ltd	+8618327326525	masar@topule.com	China	8474	58
Aladdin Scientific	+1-+1(833)-552-7181	sales@aladdinsci.com	United States	57511	58
Wuhan Jingkang en Biomedical Technology Co., Ltd	+8613720134139	orders@jknbiochem.com	China	5224	58
InvivoChem	13549236410	sales@invivochem.cn	China	6755	58
Shanghai Lollane Biological Technology Co.,Ltd.	021-52996696，15000506266 15000506266		China	4287	55

Supplier	Advantage
ATK CHEMICAL COMPANY LIMITED	60
Zhejiang J&C Biological Technology Co.,Limited	58
InvivoChem	58
Nanjing Doge Biomedical Technology Co., Ltd	58
TargetMol Chemicals Inc.	58
Wuhan Topule Biopharmaceutical Co., Ltd	58
Aladdin Scientific	58
Wuhan Jingkang en Biomedical Technology Co., Ltd	58
InvivoChem	58
Shanghai Lollane Biological Technology Co.,Ltd.	55

GSK8612 Spectrum

GSK8612(2361659-62-1)¹HNMR

2361659-62-1(GSK8612)Related Search:

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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 2361659-62-1 C17H17BrF3N7O2S