|4-(((5-溴-2-((3-甲基-1-(2,2,2-三氟乙基)-1H-吡唑-4-基)氨基)嘧啶-4-基)氨基)甲基)苯磺酰胺|CsnPharm

CAS No.: 2361659-62-1

4-(((5-Bromo-2-((3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)amino)methyl)benzenesulfonamide Catalog No. CSN24084

Synonyms: GSK 8612

GSK8612 is a potent and highly selective Tank-binding Kinase-1 (TBK1) inhibitor with pIC50 of 6.8 for recombinant TBK1.

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400-920-2911

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实验方案

技术信息

生物活性

描述GSK8612 is a novel potent and highly selective TBK1 inhibitor with an average pIC50 value of 6.8 for inhibition of recombinant TBK1 in a biochemical functional assay. It inhibited TLR3-induced IRF3 phosphorylation with an average pIC50 of 6 in poly(I:C)-stimulated Ramos cells, and inhibited IFNα secretion with an average pIC50 of 6.1 in poly(I:C)-stimulated human PBMC. GSK8612 inhibited secretion of IFNβ in THP-1 cells stimulated with dsDNA-containing virus (Baculovirus) with a pIC50 of 5.9 or cGAMP with a pIC50 of 6.3, which is the natural ligand for STING^[2].
参考文献

[1] Thomson DW, Poeckel D, et al. Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor. ACS Med Chem Lett. 2019 Mar 11;10(5):780-785.
[2] Thomson DW, Poeckel D, Zinn N, Rau C, Strohmer K, Wagner AJ, Graves AP, Perrin J, Bantscheff M, Duempelfeld B, Kasparcova V, Ramanjulu JM, Pesiridis GS, Muelbaier M, Bergamini G. Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor. ACS Med Chem Lett. 2019 Mar 11;10(5):780-785. doi: 10.1021/acsmedchemlett.9b00027. PMID: 31097999; PMCID: PMC6512007.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9219 mL
- 9.6093 mL
- 19.2187 mL
- 5 mM
- 0.3844 mL
- 1.9219 mL
- 3.8437 mL
- 10 mM
- 0.1922 mL
- 0.9609 mL
- 1.9219 mL

技术信息

CAS号

2361659-62-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H17BrF3N7O2S

运输

蓝冰

分子量

520.33

别名

GSK 8612

溶解度

DMSO	100.0 mg/mL (192.2 mM)
Water	Insoluble
Ethanol	6.0 mg/mL (11.5 mM)

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4-(((5-Bromo-2-((3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)amino)methyl)benzenesulfonamide Catalog No. CSN24084

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