GSK8612 _TBK1 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK8612Cat. No.: HY-111941CAS No.: 2361659-62-1分式: CHBrFNOS分量: 520.33作靶点: IKK作通路: NF-B储存式: -20C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 125 mg/mL (240.23 mM)* means sol

2、uble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.9219 mL 9.6093 mL 19.2186 mL5 mM 0.3844 mL 1.9219 mL 3.8437 mL10 mM 0.1922 mL 0.9609 mL 1.9219 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，

3、当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.00 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.00 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2

4、.08 mg/mL (4.00 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 GSK8612具有度选择性的，TBK1 的强效抑制剂，对重 组TBK1 的 pIC50 值为 6.8。IC50 & Target TBK16.8 (pIC50)体外研究 GSK8612 inhibits toll-like receptor (TLR)3-induced interferon regulatory factor (IRF)3 phosphorylation inRam

5、os cells and type I interferon (IFN) secretion in primary human mononuclear cells. In THP1 cells,GSK8612 is able to inhibit secretion of interferon beta (IFN ) in response to dsDNA and cGAMP, the naturalligand for STING 1.REFERENCES1. Thomson DW, et al. Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor. ACS Med Chem Lett. 2019 Mar 11;10(5):780-785.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792;