Catalog Number: 3093
Alternate 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
  • 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.
Background References
  1. Role of AMP-activated protein kinase in mechanism of metformin action.
    Zhou et al.
    J.Clin.Invest., 2001;108:1167
  2. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism.
    Yu et al.
    Nat.Chem.Biol., 2008;4:33
  3. Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway.
    Vucicevic et al.
    Autophagy, 2011;7:40
  4. Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells.
    Hao et al.
    PLoS ONE, 2008;3:2904
  5. A reliable and efficient protocol for human pluripotent stem cell differentiation into the definitive endoderm based on dispersed single cells.
    Diekmann et al.
    Stem Cells Dev., 2015;24:190
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Dorsomorphin dihydrochloride include:

33 Citations: Showing 1 - 10
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  1. Distinct and shared functions of ALS-associated proteins TDP-43, FUS and TAF15 revealed by multisystem analyses
    Authors: Kapeli Et al.
    Nature Communications 2016;7:12143
  2. Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models.
    Authors: Ahmed
    Physiological Reports 2016;4:?e13069
  3. Effects of thrombin on insulin signalling and glucose uptake in cultured human myotubes.
    Authors: Al-Bayati Et al.
    J Diabetes Complications 2016;30:1209
  4. Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
    Authors: Mou Et al.
    Cell: Stem Cell 2016;19:217
  5. Adenosine monophosphate-activated protein kinase activation mediates the leptin-induced attenuation of cognitive impairment in a streptozotocin-induced rat model.
    Authors: Zhu Et al.
    Nature 2015;9:1998
  6. Rapid and robust generation of long-term self-renewing human neural stem cells with the ability to generate mature astroglia.
    Authors: Palm Et al.
    Int J Mol Sci 2015;5:16321
  7. Transcription factor binding dynamics during human ES cell differentiation.
    Authors: Tsankov Et al.
    Biomed Res Int 2015;518:344
  8. Targeted disruption of DNMT1, DNMT3A and DNMT3B in human embryonic stem cells.
    Authors: Liao Et al.
    Exp Ther Med 2015;47:469
  9. 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.
    Authors: Sposito Et al.
    Sci Rep 2015;24:5260
  10. Comparative Study on the Cytoprotective Effects of Activated Protein C Treatment in Nonsteatotic and Steatotic Livers under Ischemia-Reperfusion Injury.
    Authors: Matsuda Et al.
    BMC Neurosci 2015;2015:635041
  11. Blocking a vicious cycle nNOS/peroxynitrite/AMPK by S-nitrosoglutathione: implication for stroke therapy.
    Authors: Khan Et al.
    J Pharmacol Exp Ther 2015;16:42
  12. Chemical constituents analysis and antidiabetic activity validation of four fern species from Taiwan.
    Authors: Chen Et al.
    Exp Neurol 2015;16:2497
  13. The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML.
    Authors: Obba Et al.
    Nat Protoc 2015;11:1114
  14. The in vitro generation of lung and airway progenitor cells from human pluripotent stem cells.
    Authors: Huang Et al.
    Nat Genet 2015;10:413
  15. Bmp suppression in mangrove killifish embryos causes a split in the body axis.
    Authors: Mourabit Et al.
    PLoS One 2014;9:e84786
  16. BMP signalling regulates the pre-implantation development of extra-embryonic cell lineages in the mouse embryo.
    Authors: Graham Et al.
    Nat Neurosci 2014;5:5667
  17. Efficient generation of lung and airway epithelial cells from human pluripotent stem cells.
    Authors: Huang Et al.
    Nat Biotechnol 2014;32:84
  18. Novel bone morphogenetic protein signaling through Smad2 and Smad3 to regulate cancer progression and development.
    Authors: Holtzhausen Et al.
    FASEB J 2014;28:1248
  19. Bmp and Shh signaling mediate the expression of satb2 in the pharyngeal arches.
    Authors: Sheehan-Rooney Et al.
    PLoS One 2013;8:e59533
  20. Derivation and expansion using only small molecules of human neural progenitors for neurodegenerative disease modeling.
    Authors: Reinhardt Et al.
    PLoS One 2013;8:e59252
  21. EGF stimulates Müller glial proliferation via a BMP-dependent mechanism.
    Authors: Ueki and Reh
    Glia 2013;61:778
  22. Moderate excess of pyruvate augments osteoclastogenesis.
    Authors: Fong Et al.
    Biol Open 2013;2:387
  23. Epigallocatechin gallate (EGCG) stimulates autophagy in vascular endothelial cells: a potential role for reducing lipid accumulation.
    Authors: Kim Et al.
    J Biol Chem 2013;288:22693
  24. Distinct energy requirements for human memory CD4 T-cell homeostatic functions.
    Authors: Taub Et al.
    Stem Cells Dev 2013;27:342
  25. Sox10-MCS5 enhancer dynamically tracks human oligodendrocyte progenitor fate.
    Authors: Pol Et al.
    Lab Chip 2013;247:694
  26. Regulation of endodermal differentiation of human embryonic stem cells through integrin-ECM interactions.
    Authors: Brafman Et al.
    Cell Metab 2013;20:369
  27. Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments.
    Authors: Li Et al.
    Nat Commun 2013;13:1969
  28. Type III TGF-β receptor promotes FGF2-mediated neuronal differentiation in neuroblastoma.
    Authors: Knelson Et al.
    J Clin Invest 2013;123:4786
  29. Liraglutide, a long-acting GLP-1 mimetic, and its metabolite attenuate inflammation after intracerebral hemorrhage.
    Authors: Hou Et al.
    J Cereb Blood Flow Metab 2012;32:2201
  30. Engineering artificial signaling centers to polarize embryoid body differentiation.
    Authors: Petersen Et al.
    Br J Pharmacol 2012;21:647
  31. Human cerebral cortex development from pluripotent stem cells to functional excitatory synapses.
    Authors: Shi Et al.
    FASEB J 2012;15:477
  32. 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
    Authors: Bumpus and Johnson
    Hum Mol Genet 2011;339:886
  33. Orexin is required for brown adipose tissue development, differentiation, and function.
    Authors: Sellayah Et al.
    Autophagy 2011;14:478
Expand to show all 33 Citations

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