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 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

Soluble to 100 mM in water and to 20 mM in DMSO with gentle warming
>98 %
Desiccate at RT

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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Safety Data Sheet: View Safety Data Sheet

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:

Al-Bayati et al (2016) Effects of thrombin on insulin signalling and glucose uptake in cultured human myotubes. J Diabetes Complications 30 1209. PMID: 27396242 .

Kapeli et al (2016) Distinct and shared functions of ALS-associated proteins TDP-43, FUS and TAF15 revealed by multisystem analyses Nature Communications 7 12143. PMID: 27378374.

Mou et al (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell: Stem Cell 19 217. PMID: 27320041.

Chen et al (2015) Chemical constituents analysis and antidiabetic activity validation of four fern species from Taiwan. Exp Neurol 16 2497. PMID: 25622260.

Huang et al (2015) The in vitro generation of lung and airway progenitor cells from human pluripotent stem cells. Nat Genet 10 413. PMID: 25654758.

Khan et al (2015) Blocking a vicious cycle nNOS/peroxynitrite/AMPK by S-nitrosoglutathione: implication for stroke therapy. J Pharmacol Exp Ther 16 42. PMID: 26174015.

Liao et al (2015) Targeted disruption of DNMT1, DNMT3A and DNMT3B in human embryonic stem cells. Exp Ther Med 47 469. PMID: 25822089.

Matsuda et al (2015) Comparative Study on the Cytoprotective Effects of Activated Protein C Treatment in Nonsteatotic and Steatotic Livers under Ischemia-Reperfusion Injury. BMC Neurosci 2015 635041. PMID: 26539519.

Obba et al (2015) The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML. Nat Protoc 11 1114. PMID: 26029847.

Palm et al (2015) Rapid and robust generation of long-term self-renewing human neural stem cells with the ability to generate mature astroglia. Int J Mol Sci 5 16321. PMID: 26541394.

Sposito et al (2015) Developmental regulation of tau splicing is disrupted in stem cell-derived neurons from frontotemporal dementia patients with the 10 + 16 splice-site mutation in MAPT. Sci Rep 24 5260. PMID: 26136155.

Tsankov et al (2015) Transcription factor binding dynamics during human ES cell differentiation. Biomed Res Int 518 344. PMID: 25693565.

Zhu et al (2015) Adenosine monophosphate-activated protein kinase activation mediates the leptin-induced attenuation of cognitive impairment in a streptozotocin-induced rat model. Nature 9 1998. PMID: 26136928.

Graham et al (2014) BMP signalling regulates the pre-implantation development of extra-embryonic cell lineages in the mouse embryo. Nat Neurosci 5 5667. PMID: 25514175.

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.

Brafman et al (2013) Regulation of endodermal differentiation of human embryonic stem cells through integrin-ECM interactions. Cell Metab 20 369. PMID: 23154389.

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.

Li et al (2013) Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments. Nat Commun 13 1969. PMID: 23563587.

Pol et al (2013) Sox10-MCS5 enhancer dynamically tracks human oligodendrocyte progenitor fate. Lab Chip 247 694. PMID: 23507034.

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.

Taub et al (2013) Distinct energy requirements for human memory CD4 T-cell homeostatic functions. Stem Cells Dev 27 342. PMID: 22972918.

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.

Petersen et al (2012) Engineering artificial signaling centers to polarize embryoid body differentiation. Br J Pharmacol 21 647. PMID: 21958075.

Shi et al (2012) Human cerebral cortex development from pluripotent stem cells to functional excitatory synapses. FASEB J 15 477. PMID: 22306606.

Bumpus and Johnson (2011) 5-Aminoimidazole-4-carboxyamide-ribonucleoside (AICAR)-stimulated hepatic expression of Cyp4a10, Cyp4a14, Cyp4a31, and other peroxisome proliferator-activated receptor α-responsive mouse genes is AICAR 5'-monophosphate-dependent and AMP-activated protein kinase-independent. Hum Mol Genet 339 886. PMID: 21896918.

Sellayah et al (2011) Orexin is required for brown adipose tissue development, differentiation, and function. Autophagy 14 478. PMID: 21982708.

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Keywords: Dorsomorphin dihydrochloride, supplier, Potent, AMPK, inhibitors, inhibits, 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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