| Bioactivity | 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]. |
| 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 hydrochloride |
| CAS | 2387510-88-3 |
| Formula | C16H16Cl2N4O2 |
| Molar Mass | 367.23 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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. |