Dorsomorphin dihydrochloride

Pricing Availability   Qty
Description: Potent AMPK inhibitor; also BMP type I receptor inhibitor
Alternative Names: Compound C,BML-275
Chemical Name: 6-[4-[2-(1-Piperidinyl)ethoxy]phenyl]-3-(4-pyridinyl)-pyrazolo[1,5-a]pyrimidine dihydrochloride
Purity: ≥98% (HPLC)
Citations (66)
Reviews (3)
Pathways (1)

Biological Activity for Dorsomorphin dihydrochloride

Dorsomorphin 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.

Compound Libraries for Dorsomorphin dihydrochloride

Dorsomorphin dihydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for Dorsomorphin dihydrochloride

M. Wt 472.41
Formula C24H25N5O.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1219168-18-9
PubChem ID 49761481
Smiles C(C=N2)(C4=CC=C(OCCN5CCCCC5)C=C4)=CN1C2=C(C3=CC=NC=C3)C=N1.Cl.Cl

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.

Solubility Data for Dorsomorphin dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 47.24 100
DMSO 9.45 20 with gentle warming

Preparing Stock Solutions for Dorsomorphin dihydrochloride

The following data is based on the product molecular weight 472.41. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.12 mL 10.58 mL 21.17 mL
5 mM 0.42 mL 2.12 mL 4.23 mL
10 mM 0.21 mL 1.06 mL 2.12 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Product Datasheets for Dorsomorphin dihydrochloride

Certificate of Analysis / Product Datasheet
Select another batch:

References for Dorsomorphin dihydrochloride

References are publications that support the biological activity of the product.

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

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

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

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

Chen et al (2019) Chemically defined neural conversion of human pluripotent stem cells. Methods Mol.Biol. 1919 59 PMID: 30656621

Guan et al (2022) Chemical reprogramming of human somatic cells to pluripotent stem cells. Nature 605 325 PMID: 35418683

Schafer et al (2023) An in vivo neuroimmune organoid model to study human microglia phenotypes. Cell 186 1222 PMID: 37172564

If you know of a relevant reference for Dorsomorphin dihydrochloride, please let us know.

View Related Products by Product Action

View all AMPK Inhibitors

Keywords: Dorsomorphin dihydrochloride, 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, differentiation, induced, pluripotent, reprogramming, iPS, Compound, C, BML-275, and, Other, Autophagy, Cardiomyocyte, Stem, Cells, ESCs, iPSC, Neural, Organoids, Cell, Reprogramming, 3093, Tocris Bioscience

66 Citations for Dorsomorphin dihydrochloride

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

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

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 Hum Mol Genet 339 886 PMID: 21896918

Schafer et al (2023) An in vivo neuroimmune organoid model to study human microglia phenotypes. Cell 186 2111 PMID: 37172564

Hsu et al (2018) Rab5 and Alsin regulate stress-activated cytoprotective signaling on mitochondria. Elife 7 PMID: 29469808

Kutsche et al (2018) Combined Experimental and System-Level Analyses Reveal the Complex Regulatory Network of miR-124 during Human Neurogenesis. Cell Syst 7 438 PMID: 30292704

Sheng et al (2018) A stably self-renewing adult blood-derived induced neural stem cell exhibiting patternability and epigenetic rejuvenation. Nat Commun 9 4047 PMID: 30279449

Rempel et al (2015) A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol 89 1599 PMID: 26272509

Ueki et al (2015) A transient wave of BMP signaling in the retina is necessary for Müller glial differentiation. Development 142 533 PMID: 25605781

Dhillon and Belsham (2011) Estrogen inhibits NPY secretion through membrane-associated estrogen receptor (ER)-α in clonal, immortalized hypothalamic neurons. Int J Obes (Lond) 35 198 PMID: 20548307

Lou et al (2011) Smarcd3b and Gata5 promote a cardiac progenitor fate in the zebrafish embryo. Development 138 3113 PMID: 21715426

Yang et al (2020) A Human Pluripotent Stem Cell-based Platform to Study SARS-CoV-2 Tropism and Model Virus Infection in Human Cells and Organoids Cell Stem Cell 27 125 PMID: 32579880

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

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

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

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

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

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

Duong et al (2012) BML-275, an AMPK inhibitor, induces DNA damage, G2/M arrest and apoptosis in human pancreatic cancer cells. Int J Oncol 41 2227 PMID: 23076030

Vershkov et al (2019) FMR1 Reactivating Treatments in Fragile X iPSC-Derived Neural Progenitors In Vitro and In Vivo. Cell Rep 26 2531 PMID: 30840878

Paonessa et al (2019) Microtubules Deform the Nuclear Membrane and Disrupt Nucleocytoplasmic Transport in Tau-Mediated Frontotemporal Dementia. Cell Rep 26 582 PMID: 30650353

Nott et al (2016) Histone deacetylase 3 associates with MeCP2 to regulate FOXO and social behavior. Nat Neurosci 19 1497 PMID: 27428650

Puente et al (2016) Nutrient-regulated Phosphorylation of ATG13 Inhibits Starvation-induced Autophagy. J Biol Chem 291 6026 PMID: 26801615

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

Yin et al (2019) Neurons Derived from Human Induced Pluripotent Stem Cells Integrate into Rat Brain Circuits and Maintain Both Excitatory and Inhibitory Synaptic Activities. Eneuro 6 PMID: 31413152

Canfield et al (2019) An isogenic neurovascular unit model comprised of human induced pluripotent stem cell-derived brain microvascular endothelial cells, pericytes, astrocytes, and neurons. Fluids Barriers CNS 16 25 PMID: 31387594

Sharma et al (2019) Exosomes regulate neurogenesis and circuit assembly. Proc Natl Acad Sci U S A 116 16086 PMID: 31320591

Jaiswal and Kimmel (2019) mTORC1/AMPK responses define a core gene set for developmental cell fate switching. BMC Biol 17 58 PMID: 31319820

Lu et al (2019) Inhibition of proliferation and migration of melanoma cells by ketoconazole and Ganoderma immunomodulatory proteins. Oncol Lett 18 891 PMID: 31289567

Ahmed (2016) Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models. Physiological Reports 4 e13069 PMID: 28039410

Park et al (2016) Ethanol extract of Kalopanax septemlobus leaf induces caspase-dependent apoptosis associated with activation of AMPK in human hepatocellular carcinoma cells. Int J Oncol 48 261 PMID: 26549816

Kottakis et al (2016) LKB1 loss links serine metabolism to DNA methylation and tumorigenesis. Nature 539 390 PMID: 27799657

Vessoni et al (2016) Cockayne syndrome-derived neurons display reduced synapse density and altered neural network synchrony. Hum Mol Genet 25 1271 PMID: 26755826

Virtanen et al (2014) Adenosine inhibits tumor cell invasion via receptor-independent mechanisms. Mol Cancer Res 12 1863 PMID: 25080434

Makanae et al (2014) Co-operative Bmp- and Fgf-signaling inputs convert skin wound healing to limb formation in urodele amphibians. Dev Biol 396 57 PMID: 25286122

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

Chen et al (2019) Chemically Defined Neural Conversion of Human Pluripotent Stem Cells Methods Mol Biol 1919 59 PMID: 30656621

Al-Bayati et al (2016) Effects of thrombin on Ins 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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Takata et al (2017) Self-patterning of rostral-caudal neuroectoderm requires dual role of Fgf signaling for localized Wnt antagonism. Nat Commun 8 1339 PMID: 29109536

Lin et al (2017) Lactate-activated macrophages induced aerobic glycolysis and epithelial-mesenchymal transition in breast cancer by regulation of CCL5-CCR5 axis: a positive metabolic feedback loop. Oncotarget 8 110426 PMID: 29299159

Morizane and Bonventre (2017) Generation of nephron progenitor cells and kidney organoids from human pluripotent stem cells. Nat Protoc 12 195 PMID: 28005067

Song et al (2017) Single-Cell Alternative Splicing Analysis with Expedition Reveals Splicing Dynamics during Neuron Differentiation. Mol Cell 67 148 PMID: 28673540

Nguyen et al (2017) DGAT1-Dependent Lipid Droplet Biogenesis Protects Mitochondrial Function during Starvation-Induced Autophagy. Dev Cell 42 9 PMID: 28697336

Dai et al (2017) Methyl-β-cyclodextrin restores impaired autophagy flux in Niemann-Pick C1-deficient cells through activation of AMPK. Autophagy 13 1435 PMID: 28613987

Caires-Júnior (2018) Discordant congenital Zika syndrome twins show differential in vitro viral susceptibility of neural progenitor cells. Nat Commun 9 475 PMID: 29396410

Gibb et al (2018) Hey2 regulates the size of the cardiac progenitor pool during vertebrate heart development. Development 145 PMID: 30355727

Do you know of a great paper that uses Dorsomorphin dihydrochloride from Tocris? Please let us know.

Reviews for Dorsomorphin dihydrochloride

Average Rating: 4.7 (Based on 3 Reviews.)

5 Star
4 Star
3 Star
2 Star
1 Star

Have you used Dorsomorphin dihydrochloride?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Filter by:

We got expected effect on cells.
By Anonymous on 04/03/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Primary pancreatic ductal epithelial cells

5 μ Dorsomorphin

review image

Neural Induction Conditions.
By Anonymous on 03/22/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: H9

2 μM dorsomorphin

PMID: 30656621
review image

Inhibition of AMP kinase in acute brain slices.
By Anonymous on 01/10/2018
Assay Type: Ex Vivo
Species: Mouse
Cell Line/Tissue: acute brain slice

On acute brain slices, to investigate the role of AMP kinase. The effect was minimal but close to what was expected.

30 minute pre-incubation

Pathways for Dorsomorphin dihydrochloride

AMPK Signaling Pathway

AMPK Signaling Pathway

AMPK signaling pathway plays an important role in the cellular reponse to low levels of available ATP, often caused by stresses such as heat shock, ischemia or hypoxia.