Stemolecule™ Dorsomorphin

Stemolecule™ Dorsomorphin

Stemolecule™ Dorsomorphin dihydrochloride is a potent inhibitor of AMP-activated protein kinase (AMPK) (Ki=109nM)¹ and bone morphogenic protein (BMP) signaling². Dorsomorphin was identified in a screen for compounds that perturb dorsoventral axis formation in zebrafish³. Dorsomorphin functions through inhibition of BMP type I receptors ALK2, ALK3 and ALK6 and thus blocks BMP-mediated SMAD1/5/8 phosphorylation³. BMP signaling coordinates developmental patterning and have essential physiological roles in mature organisms^4,5. Dorsomorphin has been used to probe BMP signaling in iron-hepcidin homeostasis³, cardiomyogenesis⁶ and osteogenesis⁷.

References

1. Gao, Y., Zhou, Y., Xu, A., Wu, D. (2008) Effects of an AMP-activated protein kinase inhibitor, compound C, on adipogenic differentiation of 3T3-L1 cells. Biol Pharm Bull 31: 1716-22.
2. Anderson, G.J., Darshan, D. (2008) Small-molecule dissection of BMP signaling. Nat Chem Biol 4: 15-6.
3. Yu, P.B., Hong, C.C., Sachidanandan, C., Babitt, J.L., Deng, D.Y., Hoyng, S.A., Lin, H.Y., Bloch, K.D., Peterson, R.T. (2008) Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat Chem Biol 4: 33-41.
4. Heisenberg, C.P., Solnica-Krezel, L. (2008) Back and forth between cell fate specification and movement during vertebrate gastrulation. Curr Opin Genet Dev 18: 311-6.
5. Cain, J.E., Hartwig, S., Bertram, J.F., Rosenblum, N.D. (2008) Bone morphogenetic protein signaling in the developing kidney: present and future. Differentiation 76: 831-42.
6. Hao, J., Daleo, M.A., Murphy, C.K., Yu, P.B., Ho, J.N., Hu, J., Peterson, R.T., Hatzopoulos, A.K., Hong, C.C. (2008) Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells. PLoS ONE 3: e2904.
7. Seib, F.P., Franke, M., Jing, D., Werner, C., Bornhauser, M. (2009) Endogenous bone morphogenetic proteins in human bone marrow-derived multipotent mesenchymal stromal cells. Eur J Cell Biol 88: 257-71.

For research use only. Not for use in diagnostic procedures. Not for resale.

Stemolecule™ Dorsomorphin

Alternate Names	6-[4-[2-(1-Piperidinyl)ethoxy]phenyl]-3-(4-pyridinyl)-p yrazolo[1,5-a]pyrimidine dihydrochloride, Compound C
Chemical Formula	C24H25N5O.2HCl.H2O
Structure
Molecular Weight	490.43
CAS Number	866405-64-3
Purity	>99%
Formulation	Yellow solid
Solubility	Soluble in DMSO (100 mM) or water (100 mM). For a 10 mM concentrated stock solution, reconstitute the compound by adding 408 µl of DMSO to the entire contents of the vial. Note: for most cells, the maximum tolerance to DMSO is <0.5%.
Storage	Store at 4°C. Protect from light. Following reconstitution, store aliquots at -20°C.
Stability	Stock solutions stable at -20°C for 6 months.
Quality control	The purity of Dorsomorphin dihydrochloride was determined by HPLC analysis. The accurate mass and structure of Dorsomorphin dihydrochloride was determined by mass spectrometry and NMR, respectively. Cellular toxicity of Dorsomorphin dihydrochloride was tested on mouse embryonic stem cells.
References	Gao, Y., Zhou, Y., Xu, A., Wu, D. (2008) Effects of an AMP-activated protein kinase inhibitor, compound C, on adipogenic differentiation of 3T3-L1 cells. Biol Pharm Bull 31: 1716-22. Anderson, G.J., Darshan, D. (2008) Small-molecule dissection of BMP signaling. Nat Chem Biol 4: 15-6. Yu, P.B., Hong, C.C., Sachidanandan, C., Babitt, J.L., Deng, D.Y., Hoyng, S.A., Lin, H.Y., Bloch, K.D., Peterson, R.T. (2008) Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat Chem Biol 4: 33-41. Heisenberg, C.P., Solnica-Krezel, L. (2008) Back and forth between cell fate specification and movement during vertebrate gastrulation. Curr Opin Genet Dev 18: 311-6. Cain, J.E., Hartwig, S., Bertram, J.F., Rosenblum, N.D. (2008) Bone morphogenetic protein signaling in the developing kidney: present and future. Differentiation 76: 831-42. Hao, J., Daleo, M.A., Murphy, C.K., Yu, P.B., Ho, J.N., Hu, J., Peterson, R.T., Hatzopoulos, A.K., Hong, C.C. (2008) Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells. PLoS ONE 3: e2904. Seib, F.P., Franke, M., Jing, D., Werner, C., Bornhauser, M. (2009) Endogenous bone morphogenetic proteins in human bone marrow-derived multipotent mesenchymal stromal cells. Eur J Cell Biol 88: 257-71.

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