OD36 is a RIPK2 inhibitor with an IC 50 of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 shows ALK2-directed activity with K D s of 37 nM.
性状
Solid
IC50 & Target[1][2]
RIPK2 5.3 nM (IC50) ACVR1 37 nM (Kd)
体外研究(In Vitro)
OD36 also inhibits ALK2 and ALK2 R206H with IC50s of 47 and 22 nM, respevtively.OD36 shows activity against ALK1 with a KD of 90 nM.OD36 potently antagonize mutant ALK2 signaling and osteogenic differentiation.OD36 (0.1-1 μM; 24 h) efficiently inhibits BMP-6 (50 ng/mL)-induced p-Smad1/5 in KS483 cells.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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
OD36 (6.25 mg/kg; i.p.; once) alleviates inflammation in an acute peritonitis mice model. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: C57BL/6 mice, muramyl dipeptide (MDP)-induced
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (100.76 mM; ultrasonic and warming and heat to 60°C)配制储备液