Chemical Name: 6-[4-[2-(1-Piperidinyl)ethoxy]phenyl]-3-(4-pyridinyl)-pyrazolo[1,5-a]pyrimidine dihydrochloride
Biological ActivityDorsomorphin dihydrochloride is a 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). Dorsomorphin dihydrochloride also inhibits bone morphogenetic protein (BMP) type I receptors (ALK2, ALK3 and ALK6), promotes cardiomyogenesis in mouse embryonic stem cells (ESCs) in vitro and promotes neural differentiation of hPSCs as part of a chemical cocktail. The compound can also be used in protocols for the chemical reprogramming of somatic cells to iPSCs.Shown to induce autophagy in cancer cell lines via a mechanism independent of AMPK inhibition. Also used in a protocol to generate brain organoids from human iPSCs.
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Role of AMP-activated protein kinase in mechanism of MetF. action.
Zhou et al.
Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism.
Yu et al.
Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway.
Vucicevic et al.
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
Citations for Dorsomorphin dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for Dorsomorphin dihydrochloride include:
66 Citations: Showing 1 - 10
An in vivo neuroimmune organoid model to study human microglia phenotypes.
Authors: Schafer Et al.
A Human Pluripotent Stem Cell-based Platform to Study SARS-CoV-2 Tropism and Model Virus Infection in Human Cells and Organoids
Authors: Yang Et al.
Cell Stem Cell 2020;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.
Microtubules Deform the Nuclear Membrane and Disrupt Nucleocytoplasmic Transport in Tau-Mediated Frontotemporal Dementia.
Authors: Paonessa Et al.
Cell Rep 2019;26:582
FMR1 Reactivating Treatments in Fragile X iPSC-Derived Neural Progenitors In Vitro and In Vivo.
Authors: Vershkov Et al.
Cell Rep 2019;26:2531
Chemically Defined Neural Conversion of Human Pluripotent Stem Cells
Authors: Chen Et al.
Methods Mol Biol 2019;1919:59
Inhibition of proliferation and migration of melanoma cells by ketoconazole and Ganoderma immunomodulatory proteins.
Authors: Lu Et al.
Oncol Lett 2019;18:891
mTORC1/AMPK responses define a core gene set for developmental cell fate switching.
Authors: Jaiswal and Kimmel
BMC Biol 2019;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 CNS 2019;16:25
Exosomes regulate neurogenesis and circuit assembly.
Authors: Sharma Et al.
Proc Natl Acad Sci U S A 2019;116:16086
A stably self-renewing adult blood-derived induced neural stem cell exhibiting patternability and epigenetic rejuvenation.
Authors: Sheng Et al.
Nat Commun 2018;9:4047
Discordant congenital Zika syndrome twins show differential in vitro viral susceptibility of neural progenitor cells.
Nat Commun 2018;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 Syst 2018;7:438
Rab5 and Alsin regulate stress-activated cytoprotective signaling on mitochondria.
Authors: Hsu Et al.
Hey2 regulates the size of the cardiac progenitor pool during vertebrate heart development.
Authors: Gibb Et al.
Self-patterning of rostral-caudal neuroectoderm requires dual role of Fgf signaling for localized Wnt antagonism.
Authors: Takata Et al.
Nat Commun 2017;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.
Single-Cell Alternative Splicing Analysis with Expedition Reveals Splicing Dynamics during Neuron Differentiation.
Authors: Song Et al.
Mol Cell 2017;67:148
DGAT1-Dependent Lipid Droplet Biogenesis Protects Mitochondrial Function during Starvation-Induced Autophagy.
Authors: Nguyen Et al.
Dev Cell 2017;42:9
Methyl-β-cyclodextrin restores impaired autophagy flux in Niemann-Pick C1-deficient cells through activation of AMPK.
Authors: Dai Et al.
Generation of nephron progenitor cells and kidney organoids from human pluripotent stem cells.
Authors: Morizane and Bonventre
Nat Protoc 2017;12:195
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
LKB1 loss links serine metabolism to DNA methylation and tumorigenesis.
Authors: Kottakis Et al.
Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models.
Physiological Reports 2016;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 Oncol 2016;48:261
Effects of thrombin on Ins signalling and glucose uptake in cultured human myotubes.
Authors: Al-Bayati Et al.
J Diabetes Complications 2016;30:1209
Nutrient-regulated Phosphorylation of ATG13 Inhibits Starvation-induced Autophagy.
Authors: Puente Et al.
J Biol Chem 2016;291:6026
Cockayne syndrome-derived neurons display reduced synapse density and altered neural network synchrony.
Authors: Vessoni Et al.
Hum Mol Genet 2016;25:1271
Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
Authors: Mou Et al.
Cell: Stem Cell 2016;19:217
Histone deacetylase 3 associates with MeCP2 to regulate FOXO and social behavior.
Authors: Nott Et al.
Nat Neurosci 2016;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.
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 Toxicol 2015;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 Sci 2015;5:16321
Transcription factor binding dynamics during human ES cell differentiation.
Authors: Tsankov Et al.
Biomed Res Int 2015;518:344
Targeted disruption of DNMT1, DNMT3A and DNMT3B in human embryonic stem cells.
Authors: Liao Et al.
Exp Ther Med 2015;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 Rep 2015;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 Neurosci 2015;2015:635041
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
Chemical constituents analysis and antidiabetic activity validation of four fern species from Taiwan.
Authors: Chen Et al.
Exp Neurol 2015;16:2497
A transient wave of BMP signaling in the retina is necessary for Müller glial differentiation.
Authors: Ueki Et al.
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
The in vitro generation of lung and airway progenitor cells from human pluripotent stem cells.
Authors: Huang Et al.
Nat Genet 2015;10:413
Bmp suppression in mangrove killifish embryos causes a split in the body axis.
Authors: Mourabit Et al.
PLoS One 2014;9:e84786
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
Co-operative Bmp- and Fgf-signaling inputs convert skin wound healing to limb formation in urodele amphibians.
Authors: Makanae Et al.
Dev Biol 2014;396:57
Efficient generation of lung and airway epithelial cells from human pluripotent stem cells.
Authors: Huang Et al.
Nat Biotechnol 2014;32:84
Novel bone morphogenetic protein signaling through Smad2 and Smad3 to regulate cancer progression and development.
Authors: Holtzhausen Et al.
FASEB J 2014;28:1248
Adenosine inhibits tumor cell invasion via receptor-independent mechanisms.
Authors: Virtanen Et al.
Mol Cancer Res 2014;12:1863
Bmp and Shh signaling mediate the expression of satb2 in the pharyngeal arches.
Authors: Sheehan-Rooney Et al.
PLoS One 2013;8:e59533
Derivation and expansion using only small molecules of human neural progenitors for neurodegenerative disease modeling.
Authors: Reinhardt Et al.
PLoS One 2013;8:e59252
EGF stimulates Müller glial proliferation via a BMP-dependent mechanism.
Authors: Ueki and Reh
Moderate excess of pyruvate augments osteoclastogenesis.
Authors: Fong Et al.
Biol Open 2013;2:387
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
Distinct energy requirements for human memory CD4 T-cell homeostatic functions.
Authors: Taub Et al.
Stem Cells Dev 2013;27:342
Sox10-MCS5 enhancer dynamically tracks human oligodendrocyte progenitor fate.
Authors: Pol Et al.
Lab Chip 2013;247:694
Regulation of endodermal differentiation of human embryonic stem cells through integrin-ECM interactions.
Authors: Brafman Et al.
Cell Metab 2013;20:369
Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments.
Authors: Li Et al.
Nat Commun 2013;13:1969
Type III TGF-β receptor promotes FGF2-mediated neuronal differentiation in neuroblastoma.
Authors: Knelson Et al.
J Clin Invest 2013;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 Oncol 2012;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 Metab 2012;32:2201
Engineering artificial signaling centers to polarize embryoid body differentiation.
Authors: Petersen Et al.
Br J Pharmacol 2012;21:647
Human cerebral cortex development from pluripotent stem cells to functional excitatory synapses.
Authors: Shi Et al.
FASEB J 2012;15:477
Estrogen inhibits NPY secretion through membrane-associated estrogen receptor (ER)-α in clonal, immortalized hypothalamic neurons.
Authors: Dhillon and Belsham
Int 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-activated
Authors: Bumpus and Johnson
Hum Mol Genet 2011;339:886
Orexin is required for brown adipose tissue development, differentiation, and function.
Authors: Sellayah Et al.
Smarcd3b and Gata5 promote a cardiac progenitor fate in the zebrafish embryo.
Authors: Lou Et al.
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