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OD36hydrochloride is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 hydrochloride is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 hydrochloride shows ALK2-directed activity with KDs of 37 nM[1][2]. | [in vivo]
OD36 (6.25 mg/kg; i.p.; once) alleviates inflammation in an acute peritonitis mice model[3]. | Animal Model: | C57BL/6 mice, muramyl dipeptide (MDP)-induced model of peritonitis[3] | | Dosage: | 6.25 mg/kg | | Administration: | Intraperitoneal injection, 30 min prior to MDP | | Result: | Inhibited the recruitment of inflammatory cells to the peritoneum, specifically that of neutrophils, and, to a lesser extent, lymphocytes. Decreased RIPK2-specific genes as well as inflammatory cytokine and chemokine gene expression.
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| [IC 50]
RIPK2: 5.3 nM (IC50); ACVR1: 37 nM (Kd); ACVR1: 47 nM (IC50); ALK2 R206H: 22 nM (IC50) | [References]
[1] Justine T Tigno-Aranjuez, et al. In vivo inhibition of RIPK2 kinase alleviates inflammatory disease. J Biol Chem. 2014 Oct 24;289(43):29651-64. DOI:10.1074/jbc.M114.591388
[2] Gonzalo Sánchez-Duffhues, et al. Development of Macrocycle Kinase Inhibitors for ALK2 Using Fibrodysplasia Ossificans Progressiva-Derived Endothelial Cells. JBMR Plus. 2019 Oct 7;3(11):e10230. DOI:10.1002/jbm4.10230
[3] Tigno-Aranjuez JT, et al. In vivo inhibition of RIPK2 kinase alleviates inflammatory disease. J Biol Chem. 2014 Oct 24;289(43):29651-64. DOI:10.1074/jbc.M114.591388 |
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