Dorsomorphin dihydrochloride

Cat. No. 3093

Dorsomorphin dihydrochloride C24H25N5O.2HCl [1219168-18-9]

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Alternative Names: Compound C, BML-275

Chemical Name: 6-[4-[2-(1-Piperidinyl)ethoxy]phenyl]-3-(4-pyridinyl)-pyrazolo[1,5-a]pyrimidine dihydrochloride

Biological Activity

Potent and selective inhibitor of AMP-activated protein kinase (AMPK) (Ki = 109 nM). Displays no significant activity on several structurally related kinases including ZAPK, SYK, PKCθ, PKA and JAK3. Inhibits AMPK activation induced by AICAR (Cat. No. 2840) and metformin (Cat. No. 2864). Also inhibits bone morphogenetic protein (BMP) type I receptors (ALK2, ALK3 and ALK6). Promotes cardiomyogenesis in mouse embryonic stem cells (ESCs) in vitro. Shown to induce autophagy in cancer cell lines via a mechanism independent of AMPK inhibition.

Technical Data

M.Wt:
472.41
Formula:
C24H25N5O.2HCl
Solubility:
Soluble to 100 mM in water and to 20 mM in DMSO with gentle warming
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
1219168-18-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Diekmann et al (2015) A reliable and efficient protocol for human pluripotent stem cell differentiation into the definitive endoderm based on dispersed single cells. Stem Cells Dev. 24 190. PMID: 25137387.

Vucicevic et al (2011) Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway. Autophagy 7 40. PMID: 20980833.

Hao et al (2008) Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells. PLoS ONE 3 2904. PMID: 18682835.

Yu et al (2008) Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat.Chem.Biol. 4 33. PMID: 18026094.

Zhou et al (2001) Role of AMP-activated protein kinase in mechanism of metformin action. J.Clin.Invest. 108 1167. PMID: 11602624.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Dorsomorphin dihydrochloride include:

Holtzhausen et al (2014) Novel bone morphogenetic protein signaling through Smad2 and Smad3 to regulate cancer progression and development. FASEB J 28 1248. PMID: 24308972.

Huang et al (2014) Efficient generation of lung and airway epithelial cells from human pluripotent stem cells. Nat Biotechnol 32 84. PMID: 24291815.

Mourabit et al (2014) Bmp suppression in mangrove killifish embryos causes a split in the body axis. PLoS One 9 e84786. PMID: 24497921.

Fong et al (2013) Moderate excess of pyruvate augments osteoclastogenesis. Biol Open 2 387. PMID: 23616923.

Kim et al (2013) Epigallocatechin gallate (EGCG) stimulates autophagy in vascular endothelial cells: a potential role for reducing lipid accumulation. J Biol Chem 288 22693. PMID: 23754277.

Knelson et al (2013) Type III TGF-β receptor promotes FGF2-mediated neuronal differentiation in neuroblastoma. J Clin Invest 123 4786. PMID: 24216509.

Reinhardt et al (2013) Derivation and expansion using only small molecules of human neural progenitors for neurodegenerative disease modeling. PLoS One 8 e59252. PMID: 23533608.

Sheehan-Rooney et al (2013) Bmp and Shh signaling mediate the expression of satb2 in the pharyngeal arches. PLoS One 8 e59533. PMID: 23555697.

Ueki and Reh (2013) EGF stimulates Müller glial proliferation via a BMP-dependent mechanism. Glia 61 778. PMID: 23362023.

Hou et al (2012) Liraglutide, a long-acting GLP-1 mimetic, and its metabolite attenuate inflammation after intracerebral hemorrhage. J Cereb Blood Flow Metab 32 2201. PMID: 22968320.

Do you know of a great paper that uses Dorsomorphin dihydrochloride from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: Dorsomorphin dihydrochloride, supplier, Potent, selective, AMPK, inhibitors, BMP, type, I, receptor, ALK2, ALK3, ALK6, AMP-Activated, Protein, Kinases, Receptors, Activin, Receptor-like, Receptor, Serine/Threonine, RSTKs, stem, cells, BML275, 866405-64-3, Tocris Bioscience, AMPK Inhibitor products

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