General description
A cell-permeable, potent, and highly selective BMPR (bone morphogenetic protein receptor) inhibitior (IC50 against human ALK2/BMPR-I = 107.9 nM) that exhibits no inhibitory activity against ALK5, AMPK, FLK1/KDR/VEGRF2, or PDGFRβ. Effectively blocks ALK2- and ALK3-, but not ALK6-, mediated transcription activity (IC50﹤500 nM, ﹤100 nM, and >10 M in reporter assays using C2C12BRA expressing constitutively active ALK2, ALK3, or ALK6, respectively). Comparing to its non-BMPR-selective structural analog dorsomorphin, DMH1 is 12.5-times more potent in preventing BMP pathway-dependent DV (dorsoventral) development (EC100 = 0.2 M DMH1 or 2.5 M DM) in zebrafish embryo in vivo, while being non-toxic to the fish embryo and exhibiting no effect against VEGF signaling-dependent intersomitic vessel (ISV) formation even at concentrations as high as 50 M.
A cell-permeable, potent, and highly selective BMPR inhibitior (IC50 against human ALK2/BMPR-I = 107.9 nM), exhibiting no activity toward ALK5, ALK6, AMPK, FLK1/KDR/VEGRF2, or PDGFRβ. Comparing to its non-BMPR-selective structural analog dorsomorphin DMH1 is 12.5-times more potent in preventing BMP pathway-dependent dorsoventral development (EC100 = 0.2 M) in zebrafish embryo in vivo, while being non-toxic to the fish embryo and exhibiting no effect against VEGF signaling-dependent intersomitic vessel formation even at concentrations as high as 50 M.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Hao, J., et al. 2010. ACS Chem.Biol.5, 245.
Packaging
5 mg in Glass bottle
Packaged under inert gas
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Warning
Toxicity: Regulatory Review (Z)
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