GSK2983559 is an orally active and potent receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 blocks many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.
性状
Solid
IC50 & Target[1][2]
RIPK2
体外研究(In Vitro)
GSK2983559 (1-1024 nM; 2 h) blocks MDP-induced IL-8 in THP-1 cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
GSK2983559 (oral gavage; 3 and 10 mg/kg; once) inhibits effectively MDP-induced IL-6 in mouse. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: C57BL/6 mice (female) injected with MDP
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Pamela A Haile, et al. Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inf[2]. Shuwei Wu, et al. Design, synthesis, and structure-activity relationship of novel RIPK2 inhibitors. Bioorg Med Chem Lett. 2022 Sep 2;75:128968.
溶解度数据
In Vitro: H2O : 2 mg/mL (3.27 mM; Need ultrasonic)DMSO : < 1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble or slightly soluble)DMF : < 1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble)Ethanol : < 1 mg/mL (ultrasonic) (insoluble)