GSK8612 _TBK1 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK8612Cat. No.: HY-111941CAS No.: 2361659-62-1分式: CHBrFNOS分量: 520.33作靶點: IKK作通路: NF-B儲存式: -20C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (240.23 mM)* means sol

2、uble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，

3、當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.00 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.00 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2

4、.08 mg/mL (4.00 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 GSK8612具有度選擇性的，TBK1 的強(qiáng)效抑制劑，對重 組TBK1 的 pIC50 值為 6.8。IC50 & Target TBK16.8 (pIC50)體外研究 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;