GSK2983559

• CAT Number: I046166
• Molecular Formula: C21H23N4O7PS2.1/2Ca.3H2O
• Molecular Weight: 612.63
• Purity: ≥95%

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[1].
GSK2983559 (1-1024 nM; 2 h) blocks MDP-induced IL-8 in THP-1 cells[2].
GSK2983559 (oral gavage; 3 and 10 mg/kg; once) inhibits effectively MDP-induced IL-6 in mouse[2].

Reference

[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 Inflammatory Diseases. J Med Chem. 2019 Jul 25;62(14):6482-6494.
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[2]. Shuwei Wu, et al. Design, synthesis, and structure-activity relationship of novel RIPK2 inhibitors. Bioorg Med Chem Lett. 2022 Sep 2;75:128968.
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