产品说明书

GSK8612

Print
Chemical Structure| 2361659-62-1 同义名 : -
CAS号 : 2361659-62-1
货号 : A1149118
分子式 : C17H17BrF3N7O2S
纯度 : 99%+
分子量 : 520.327
MDL号 : MFCD32062739
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(230.62 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.61mL

1.92mL

0.96mL

19.22mL

3.84mL

1.92mL
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.