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. Promotes neural differentiation of hPSCs as part of a chemical cocktail. Shown to induce autophagy in cancer cell lines via a mechanism independent of AMPK inhibition.Technical Data
The technical data provided above is for guidance only.For batch specific data refer to the Certificate of Analysis.Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
- Role of AMP-activated protein kinase in mechanism of MetF. action.Zhou et al.J.Clin.Invest., 2001;108:1167
- Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism.Yu et al.Nat.Chem.Biol., 2008;4:33
- Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway.Vucicevic et al.Autophagy, 2011;7:40
- Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells.Hao et al.PLoS ONE, 2008;3:2904
- 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
- Chemically defined neural conversion of human pluripotent stem cells.Chen et al.Methods Mol.Biol., 2019;1919:59
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Citations for Dorsomorphin dihydrochloride
The citations listed below are publications that use Tocris products.Selected citations for Dorsomorphin dihydrochloride include:
65Citations: Showing 1 - 10
- A Human Pluripotent Stem Cell-based Platform to Study SARS-CoV-2 Tropism and Model Virus Infection in Human Cells and OrganoidsAuthors: Yang Et al.Cell Stem Cell2020;27:125
- Neurons Derived from Human Induced Pluripotent Stem Cells Integrate into Rat Brain Circuits and Maintain Both Excitatory and Inhibitory Synaptic Activities.Authors: Yin Et al.Eneuro2019;6
- Microtubules Deform the Nuclear Membrane and Disrupt Nucleocytoplasmic Transport in Tau-Mediated Frontotemporal Dementia.Authors: Paonessa Et al.Cell Rep2019;26:582
- FMR1 Reactivating Treatments in Fragile X iPSC-Derived Neural Progenitors In Vitro and In Vivo.Authors: Vershkov Et al.Cell Rep2019;26:2531
- Chemically Defined Neural Conversion of Human Pluripotent Stem CellsAuthors: Chen Et al.Methods Mol Biol2019;1919:59
- Inhibition of proliferation and migration of melanoma cells by ketoconazole and Ganoderma immunomodulatory proteins.Authors: Lu Et al.Oncol Lett2019;18:891
- mTORC1/AMPK responses define a core gene set for developmental cell fate switching.Authors: Jaiswal and KimmelBMC Biol2019;17:58
- An isogenic neurovascular unit model comprised of human induced pluripotent stem cell-derived brain microvascular endothelial cells, pericytes, astrocytes, and neurons.Authors: Canfield Et al.Fluids Barriers CNS2019;16:25
- Exosomes regulate neurogenesis and circuit assembly.Authors: Sharma Et al.Proc Natl Acad Sci U S A2019;116:16086
- A stably self-renewing adult blood-derived induced neural stem cell exhibiting patternability and epigenetic rejuvenation.Authors: Sheng Et al.Nat Commun2018;9:4047
- Discordant congenital Zika syndrome twins show differential in vitro viral susceptibility of neural progenitor cells.Authors: Caires-J?niorNat Commun2018;9(1):475
- Combined Experimental and System-Level Analyses Reveal the Complex Regulatory Network of miR-124 during Human Neurogenesis.Authors: Kutsche Et al.Cell Syst2018;7:438
- Rab5 and Alsin regulate stress-activated cytoprotective signaling on mitochondria.Authors: Hsu Et al.Elife2018;7
- Hey2 regulates the size of the cardiac progenitor pool during vertebrate heart development.Authors: Gibb Et al.Development2018;145
- Self-patterning of rostral-caudal neuroectoderm requires dual role of Fgf signaling for localized Wnt antagonism.Authors: Takata Et al.Nat Commun2017;8:1339
- Lactate-activated macrophages induced aerobic glycolysis and epithelial-mesenchymal transition in breast cancer by regulation of CCL5-CCR5 axis: a positive metabolic feedback loop.Authors: Lin Et al.Oncotarget2017;8:110426
- Single-Cell Alternative Splicing Analysis with Expedition Reveals Splicing Dynamics during Neuron Differentiation.Authors: Song Et al.Mol Cell2017;67:148
- DGAT1-Dependent Lipid Droplet Biogenesis Protects Mitochondrial Function during Starvation-Induced Autophagy.Authors: Nguyen Et al.Dev Cell2017;42:9
- Methyl-β-cyclodextrin restores impaired autophagy flux in Niemann-Pick C1-deficient cells through activation of AMPK.Authors: Dai Et al.Autophagy2017;13:1435
- Generation of nephron progenitor cells and kidney organoids from human pluripotent stem cells.Authors: Morizane and BonventreNat Protoc2017;12:195
- Distinct and shared functions of ALS-associated proteins TDP-43, FUS and TAF15 revealed by multisystem analysesAuthors: Kapeli Et al.Nature Communications2016;7:12143
- LKB1 loss links serine metabolism to DNA methylation and tumorigenesis.Authors: Kottakis Et al.Nature2016;539:390
- Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models.Authors: AhmedPhysiological Reports2016;4:e13069
- Ethanol extract of Kalopanax septemlobus leaf induces caspase-dependent apoptosis associated with activation of AMPK in human hepatocellular carcinoma cells.Authors: Park Et al.Int J Oncol2016;48:261
- Effects of thrombin on Ins signalling and glucose uptake in cultured human myotubes.Authors: Al-Bayati Et al.J Diabetes Complications2016;30:1209
- Nutrient-regulated Phosphorylation of ATG13 Inhibits Starvation-induced Autophagy.Authors: Puente Et al.J Biol Chem2016;291:6026
- Cockayne syndrome-derived neurons display reduced synapse density and altered neural network synchrony.Authors: Vessoni Et al.Hum Mol Genet2016;25:1271
- Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal CellsAuthors: Mou Et al.Cell: Stem Cell2016;19:217
- Histone deacetylase 3 associates with MeCP2 to regulate FOXO and social behavior.Authors: Nott Et al.Nat Neurosci2016;19:1497
- Adenosine monophosphate-activated protein kinase activation mediates the leptin-induced attenuation of cognitive impairment in a streptozotocin-induced rat model.Authors: Zhu Et al.Nature2015;9:1998
- A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors.Authors: Rempel Et al.Arch Toxicol2015;89:1599
- 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 Sci2015;5:16321
- Transcription factor binding dynamics during human ES cell differentiation.Authors: Tsankov Et al.Biomed Res Int2015;518:344
- Targeted disruption of DNMT1, DNMT3A and DNMT3B in human embryonic stem cells.Authors: Liao Et al.Exp Ther Med2015;47:469
- 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 Rep2015;24:5260
- 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 Neurosci2015;2015:635041
- Blocking a vicious cycle nNOS/peroxynitrite/AMPK by S-nitrosoglutathione: implication for stroke therapy.Authors: Khan Et al.J Pharmacol Exp Ther2015;16:42
- Chemical constituents analysis and antidiabetic activity validation of four fern species from Taiwan.Authors: Chen Et al.Exp Neurol2015;16:2497
- A transient wave of BMP signaling in the retina is necessary for Müller glial differentiation.Authors: Ueki Et al.Development2015;142:533
- The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML.Authors: Obba Et al.Nat Protoc2015;11:1114
- The in vitro generation of lung and airway progenitor cells from human pluripotent stem cells.Authors: Huang Et al.Nat Genet2015;10:413
- Bmp suppression in mangrove killifish embryos causes a split in the body axis.Authors: Mourabit Et al.PLoS One2014;9:e84786
- BMP signalling regulates the pre-implantation development of extra-embryonic cell lineages in the mouse embryo.Authors: Graham Et al.Nat Neurosci2014;5:5667
- Co-operative Bmp- and Fgf-signaling inputs convert skin wound healing to limb formation in urodele amphibians.Authors: Makanae Et al.Dev Biol2014;396:57
- Efficient generation of lung and airway epithelial cells from human pluripotent stem cells.Authors: Huang Et al.Nat Biotechnol2014;32:84
- Novel bone morphogenetic protein signaling through Smad2 and Smad3 to regulate cancer progression and development.Authors: Holtzhausen Et al.FASEB J2014;28:1248
- Adenosine inhibits tumor cell invasion via receptor-independent mechanisms.Authors: Virtanen Et al.Mol Cancer Res2014;12:1863
- Bmp and Shh signaling mediate the expression of satb2 in the pharyngeal arches.Authors: Sheehan-Rooney Et al.PLoS One2013;8:e59533
- Derivation and expansion using only small molecules of human neural progenitors for neurodegenerative disease modeling.Authors: Reinhardt Et al.PLoS One2013;8:e59252
- EGF stimulates Müller glial proliferation via a BMP-dependent mechanism.Authors: Ueki and RehGlia2013;61:778
- Moderate excess of pyruvate augments osteoclastogenesis.Authors: Fong Et al.Biol Open2013;2:387
- Epigallocatechin gallate (EGCG) stimulates autophagy in vascular endothelial cells: a potential role for reducing lipid accumulation.Authors: Kim Et al.J Biol Chem2013;288:22693
- Distinct energy requirements for human memory CD4 T-cell homeostatic functions.Authors: Taub Et al.Stem Cells Dev2013;27:342
- Sox10-MCS5 enhancer dynamically tracks human oligodendrocyte progenitor fate.Authors: Pol Et al.Lab Chip2013;247:694
- Regulation of endodermal differentiation of human embryonic stem cells through integrin-ECM interactions.Authors: Brafman Et al.Cell Metab2013;20:369
- Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments.Authors: Li Et al.Nat Commun2013;13:1969
- Type III TGF-β receptor promotes FGF2-mediated neuronal differentiation in neuroblastoma.Authors: Knelson Et al.J Clin Invest2013;123:4786
- BML-275, an AMPK inhibitor, induces DNA damage, G2/M arrest and apoptosis in human pancreatic cancer cells.Authors: Duong Et al.Int J Oncol2012;41:2227
- LirGlu., a long-acting GLP-1 mimetic, and its metabolite attenuate inflammation after intracerebral hemorrhage.Authors: Hou Et al.J Cereb Blood Flow Metab2012;32:2201
- Engineering artificial signaling centers to polarize embryoid body differentiation.Authors: Petersen Et al.Br J Pharmacol2012;21:647
- Human cerebral cortex development from pluripotent stem cells to functional excitatory synapses.Authors: Shi Et al.FASEB J2012;15:477
- Estrogen inhibits NPY secretion through membrane-associated estrogen receptor (ER)-α in clonal, immortalized hypothalamic neurons.Authors: Dhillon and BelshamInt J Obes (Lond)2011;35:198
- 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-activatedAuthors: Bumpus and JohnsonHum Mol Genet2011;339:886
- Orexin is required for brown adipose tissue development, differentiation, and function.Authors: Sellayah Et al.Autophagy2011;14:478
- Smarcd3b and Gata5 promote a cardiac progenitor fate in the zebrafish embryo.Authors: Lou Et al.Development2011;138:3113
FAQs
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Human AMPK alpha 2 (NP_006243) VersaClone cDNA
Human AMPK alpha 1 (NP_006242) VersaClone cDNA
Human AMPK beta 1 (NP_006244) VersaClone cDNA
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On acute brain slices, to investigate the role of AMP kinase. The effect was minimal but close to what was expected.
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