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RIPK2 inhibitor OD36 is an inhibitor of receptor-interacting serine/threonine kinase 2 (RIPK2; IC50 = 5.3 nM).1 It also inhibits wild-type and R206H mutant activin receptor-like kinase 2 (ALK2; IC50s = 47 and 22 nM, respectively).2 RIPK2 inhibitor OD36 (0.5 µM) inhibits activin A-induced chondrogenic and osteogenic differentiation in ATDC-5 cells overexpressing ALKR206H, an activating mutation found in patients with fibrodysplasia ossificans progressiva (FOP), which is characterized by progressive heterotopic ossification, or diffuse intrinsic pontine glioma (DIPG), a type of pediatric brain stem cancer. In vivo, RIPK2 inhibitor OD36 (6.25 mg/kg) reduces the number of peritoneal lavage neutrophils and lymphocytes in a mouse model of muramyl dipeptide-induced peritonitis.1
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1. In vivo inhibition of RIPK2 kinase alleviates inflammatory disease. The Journal of Biological Chemisty 289(43), 29651-29664 (2014).
2. Development of macrocycle kinase inhibitors for ALK2 using fibrodysplasia ossificans progressiva-