DMH1

Bone morphogenetic proteins (BMP) are secreted signaling proteins, many of which are involved in various developmental processes, in addition to bone formation.¹ DMH1 is an analog of the non-selective BMP receptor inhibitor dorsomorphin (Item No. 11967) that potently inhibits the kinase activity of activin receptor-like kinase 2 (ALK2; IC₅₀ = 13-108 nM).^2,3 It is much less effective at ALK4, ALK5, AMPK, KDR (VEGFR2) or PDGFRβ, although it inhibits ALK1 and ALK3 at nanomolar concentrations.^2,3 DMH1 is effective in vivo, as it disrupts dorsoventral development in zebrafish.² It also affects stem cell development, increasing cardiomyocyte progenitors and promoting neurogenesis.^4,5 DMH1 inhibits the growth of lung cancer cells, reducing tumor growth in a xenograft mouse model.⁶

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1. Sakata, T., and Chen, J.K. Chemical 'Jekyll and Hyde’s: Small-molecule inhibitors of developmental signaling pathways. Chem. Soc. Rev. 40(8), 4318-4331 (2011).

2. Hao, J., Ho, J.N., Lewis, J.A., et al. In vivo structure activity relationship study of dorsomorphin analogs identifies selective VEGF and BMP inhibitors. ACS Chem. Biol. 5(2), 245-253 (2010).

3. Mohedas, A.H., Xing, X., Armstrong, K.A., et al. Development of an ALK2-biased BMP type I receptor kinase inhibitor. ACS Chem. Biol. 8(6), 1291-1302 (2013).

4. Ao, A., Hao, J., Hopkins, C.R., et al. DMH1, a novel BMP small molecule inhibitor, increases cardiomyocyte progenitors and promotes cardiac differentiation in mouse embryonic stem cells. PLoS One 7(7), e41627 (2012).

5. Neely, M.D., Litt, M.J., Tidball, A.M., et al. DMH1, a highly selective small molecule BMP inhibitor promotes neurogenesis of hiPSCs: Comparison of PAX6 and SOX1 expression during neural induction. ACS Chem. Neurosci. 3(6), 482-491 (2012).

6. Hao, J., Lee, R., Chang, A., et al. DMH1, a small molecule inhibitor of BMP type I receptors, suppresses growth and invasion of lung cancer. PLoS One 9(3), 1-6 (2014).