OD36
目录号: PL11010 纯度: ≥98%
CAS No. :1638644-62-8
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中文名称
OD36
英文名称
OD36
英文别名
Cyclical Inhibitor Od36;OD 36;B4E;OD36
Cas No.
1638644-62-8
分子式
C16H15ClN4O2
分子量
330.77
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
OD36 是一种 RIPK2 抑制剂,IC50 为 5.3 nM。OD36 是一种大环抑制剂,可与 ALK2 激酶 ATP 口袋有效结合。OD36 靶向作用于 ALK2,KD 为 37 nM。
生物活性
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
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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