Bone morphogenetic proteins (BMP) are secreted signaling proteins, many of which are involved in various developmental processes, in addition to bone formation. DMH1 is an analog of the non-selective BMP receptor inhibitor dorsomorphin. that potently inhibits the kinase activity of activin receptor-like kinase 2 (ALK2; IC50 = 13-108 nM). It is much less effective at ALK4, ALK5, AMPK, KDR (VEGFR2) or PDGFRβ, although it inhibits ALK1 and ALK3 at nanomolar concentrations. DMH1 is effective in vivo, as it disrupts dorsoventral development in zebrafish. It also affects stem cell development, increasing cardiomyocyte progenitors and promoting neurogenesis. DMH1 inhibits the growth of lung cancer cells, reducing tumor growth in a xenograft mouse model.
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