K02288 is an inhibitor of type I BMP receptor. It targeting ALK2, ALK1 and ALK6 with IC50 of 1.1, 1.8, 6.4 nM, respectively.
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Bone morphogenetic proteins (BMPs), members of the TGFβ superfamily, play an important role in stem cell biology and function to regulate cell proliferation and differentiation during development. BMPs initiate their signaling events through an interaction of their type I and type II receptors, both of which are transmembrane serine/threonine kinases. Seven type I receptors (a.k.a. activin receptor-like receptors; ALK1 to ALK7) and four type II receptors have been identified in mice and humans[3]. K02288 is a potent BMP type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 also shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM. Furthermore, K02288 further demonstrated an improved selectivity against ALK4 and ALK5 with IC50s of 321 nM and 302 nM, respectively. In C2C12 cells, the phosphorylation of Smad1/5/8, induced by BMP4, can be reduced by K02288 in a dose dependent manner with an apparent IC50 of 100 nM [4]. In LX-2 cells, the proliferation promotion effect of BMP9 stimulation was inhibited by incubating with 1μM of K02288 for 4 hours. In addition, the expression of pSMAD1/5, ID1, and α-SMA were significantly decreased by K02288 treatment[5]. On embryo development day 6, 100μl of K02288 (1μM) was deposited on the chick embryo chorioallantoic membrane (CAM) model. Four days later, a large fraction of the CAM models exhibited a distinctive phenotype of low vessel density reflecting the dysfunctional angiogenesis which occurs following hypersprouting[1].
作用机制
K02288 binds type I BMP receptor at the ATP-binding pocket. The 2-aminopyridine group of K02288 is an ATP-mimetic that binds the kinase hinge region of type I BMP receptor through two conserved hydrogen bonds[4].
K02288 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
HEK293T cells
Function assay
30 mins
Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay, IC50=3.4 μM
25101911
mouse C2C12 cells
Function assay
30 mins
Inhibition of BMP2-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay, IC50=0.23 μM
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