| Bioactivity | OD36 is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 shows ALK2-directed activity with KDs of 37 nM[1][2]. | ||||||||||||
| Invitro | OD36 also inhibits ALK2 and ALK2 R206H with IC50s of 47 and 22 nM, respevtively[1].OD36 shows activity against ALK1 with a KD of 90 nM[2].OD36 potently antagonize mutant ALK2 signaling and osteogenic differentiation[2].OD36 (0.1-1 μM; 24 h) efficiently inhibits BMP-6 (50 ng/mL)-induced p-Smad1/5 in KS483 cells[2].Preincubation of fibrodysplasia ossificans progressiva (FOP) endothelial colony-forming cells (ECFCs) with OD36 (0.5 μM) completely prevents the activation of Smad1/5 and gene targets ID-1 and ID-3 in response to activin A[2]. Western Blot Analysis[2] Cell Line: | ||||||||||||
| In Vivo | OD36 (6.25 mg/kg; i.p.; once) alleviates inflammation in an acute peritonitis mice model[3]. Animal Model: | ||||||||||||
| Name | OD36 | ||||||||||||
| CAS | 1638644-62-8 | ||||||||||||
| Formula | C16H15ClN4O2 | ||||||||||||
| Molar Mass | 330.77 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [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. [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. |