K 02288;3-[6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenol;K02288;K-02288;3-[(6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenol;3-[6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]-phenol;3-[6-Amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenol;K02288;3-(6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenol;A3F;SYN5187;AOB4291;HMS3653M16;BDBM102619;K02288a;BCP09946;s7359;K 02288a;FD5034;SB19486;BC600483;AK175599;Y1876;K02288, >98% (HPLC);SW220200-1;A14311;Phenol
K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC 50 s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC 50 s of of 5-34 nM.
K02288 reduces a robust phosphorylation of Smad1/5/8 induced by BMP4 stimulation, with an apparent IC50 of 100 nM. K02288 causes near complete inhibition of Smad2 phosphorylation at 0.5 μM. K02288 binds to ALK1 in an ATP-mimetic fashion with two hydrogen bonds to the kinase hinge. K02288 also inhibits BMP9-ALK1 signalling, and induces a hypersprouting phenotype in HUVECs. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
K02288 (1 μM) induces dysfunctional angiogenesis in a chick embryo CAM model. has not independently confirmed the accuracy of these methods. They are for reference only.
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]. Sanvitale CE, et al. A new class of small molecule inhibitor of BMP signaling. PLoS One. 2013 Apr 30;8(4):e62721.[2]. Kerr G, et al. A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis. Angiogenesis. 2015 Apr;18(2):209-17.