PeptideDB

GSK2983559 free acid

CAS: 1579965-12-0 F: C21H23N4O7PS2 W: 538.53

GSK2983559 free acid (compound 3) is an orally active and potent receptor interacting protein 2 (RIP2) kinase inhibitor.
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Bioactivity GSK2983559 free acid (compound 3) is an orally active and potent receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid can block many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples[1].
Invitro GSK2983559 (1-1024 nM; 2 h) blocks MDP-induced IL-8 in THP-1 cells[2]. Cell Viability Assay[2] Cell Line:
In Vivo GSK2983559 (oral gavage; 3 and 10 mg/kg; once) inhibits effectively MDP-induced IL-6 in mouse[2]. Animal Model:
Name GSK2983559 free acid
CAS 1579965-12-0
Formula C21H23N4O7PS2
Molar Mass 538.53
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Reference [1]. Haile PA, 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 Inflammat [2]. Shuwei Wu, et al. Design, synthesis, and structure-activity relationship of novel RIPK2 inhibitors. Bioorg Med Chem Lett. 2022 Sep 2;75:128968.