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Submit ReviewDMH-1
Description: Selective ALK2 inhibitor
Chemical Name: 4-[6-[4-(1-Methylethoxy)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline
Purity: ≥98% (HPLC)
Biological Activity for DMH-1
DMH-1 is a selective inhibitor of bone morphogenic protein (BMP) type-I receptor activin receptor-like kinase 2 (ALK2) receptor (IC50 = 108 nM or 12.6 nM in in vitro kinase assays). DMH-1 exhibits 6- and 19-fold selectivity for ALK-2 over ALK-1 and ALK-3, respectively, and no significant inhibition of AMPK, ALK5, KDR (VEGFR-2) or PDGFRβ receptors. DMH-1 blocks BMP4-induced phosphorylation of Smads 1, 5 and 8 in HEK293 cells. Promotes neurogenesis in human induced pluripotent stem cells (iPSCs) when used in combination with SB 431542 (Cat. No. 1614). DMH-1 suppresses lung cancer cell proliferation, migration, invasion in vitro and reduces tumor growth in a mouse lung cancer xenograft model. DMH-1 inhibits cellular autophagy responses. DMH-1 induces intestinal differentiation in human intestinal organoids (hIOs) derived from human pluripotent stems cells (hPSCs). The compound can also be used in protocols for the chemical reprogramming of somatic cells to iPSCs.
Compound Libraries for DMH-1
DMH-1 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for DMH-1
| M. Wt | 380.44 |
| Formula | C24H20N4O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1206711-16-1 |
| PubChem ID | 50997747 |
| InChI Key | JMIFGARJSWXZSH-UHFFFAOYSA-N |
| Smiles | CC(C)OC(C=C3)=CC=C3C(C=N2)=CN1C2=C(C4=CC=NC5=C4C=CC=C5)C=N1 |
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 DMH-1
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.61 | 20 |
Preparing Stock Solutions for DMH-1
The following data is based on the product molecular weight 380.44. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 13.14 mL | 65.71 mL | 131.43 mL |
| 1 mM | 2.63 mL | 13.14 mL | 26.29 mL |
| 2 mM | 1.31 mL | 6.57 mL | 13.14 mL |
| 10 mM | 0.26 mL | 1.31 mL | 2.63 mL |
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Product Datasheets for DMH-1
References for DMH-1
References are publications that support the biological activity of the product.
Bowman and Zon (2010) Swimming into the future of drug discovery: in vivo chemical screens in zebrafish. ACS Chem.Biol. 5 159 PMID: 20166761
Hao et al (2010) In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. ACS Chem.Biol. 5 245 PMID: 20020776
Neely et al (2012) DMH1, a highly selective small molecule BMP inhibitor, promotes neurogenesis of hiPSCs: comparison of PAX6 and SOX1 expression during neural induction. ACS Chem.Neurosci. 3 482 PMID: 22860217
Mohedas et al (2013) Development of an ALK2-biased BMP type I receptor kinase inhibitor. ACS Chem.Biol. 8 1291 PMID: 23547776
Hao et al (2014) DMH1, a small molecule inhibitor of BMP type i receptors, suppresses growth and invasion of lung cancer. PLoS One 9 e90748 PMID: 24603907
Sheng et al (2015) DMH1 (4-[6-(4-isopropoxyphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline) inhibits chemotherapeutic drug-induced autophagy. Acta Pharmacol.Sinica 5 330 PMID: 26579463
Jung et al (2018) In vitro and in vivo imaging and tracking of intestinal organoids from human induced pluripotent stem cells. FASEB J. 32 111 PMID: 28855280
Guan et al (2022) Chemical reprogramming of human somatic cells to pluripotent stem cells. Nature 605 325 PMID: 35418683
If you know of a relevant reference for DMH-1, please let us know.
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Keywords: DMH-1, DMH-1 supplier, selective, activin, receptors, alk2, acvr1, bmp, type, I, bone, morphogenic, morphogenetic, protein, iPSC, neurogenesis, antiproliferative, differentiation, organoid, induced, pluripotent, stem, cells, reprogramming, BMP, and, Other, Activin, Receptors, ESCs, Stem, Cell, Reprogramming, 4126, Tocris Bioscience
50 Citations for DMH-1
Citations are publications that use Tocris products. Selected citations for DMH-1 include:
Mark et al (2023) Axon guidance genes modulate neurotoxicity of ALS-associated UBQLN2. Elife 12 PMID: 37039476
Thaddeus G et al (2020) In Vitro CRISPR/Cas9-Directed Gene Editing to Model LRRK2 G2019S Parkinson's Disease in Common Marmosets. Sci Rep 10 3447 PMID: 32103062
Lee J et al (2020) DNA damage accumulates and responses are engaged in human ALS brain and spinal motor neurons and DNA repair is activatable in iPSC-derived motor neurons with SOD1 mutations. Acta Neuropathol Commun 8 7 PMID: 32005289
Gerald I et al (2020) The omentum of obese girls harbors small adipocytes and browning transcripts. JCI Insight 5 PMID: 32125283
Erik M et al (2020) Multiplatform genomic profiling and magnetic resonance imaging identify mechanisms underlying intratumor heterogeneity in meningioma. Nat Commun 11 4803 PMID: 32968068
Lee J et al (2020) Human Motor Neurons With SOD1-G93A Mutation Generated From CRISPR/Cas9 Gene-Edited iPSCs Develop Pathological Features of Amyotrophic Lateral Sclerosis. Front Cell Neurosci 14 604171 PMID: 33328898
Jason et al (2020) Generation and trapping of a mesoderm biased state of human pluripotency. Nat Commun 11 4989 PMID: 33020476
Kimberly J et al (2020) BMP signaling plays a role in anterior-neural/head development, but not organizer activity, in the gastropod Crepidula fornicata. Dev Biol 463 135-157 PMID: 32389712
Jianming et al (2020) Human Bocavirus 1 Infection of Well-Differentiated Human Airway Epithelium. Curr Protoc Microbiol 58 e107 PMID: 32639683
Vermilyea et al (2017) Induced Pluripotent Stem Cell-Derived Dopaminergic Neurons from Adult Common Marmoset Fibroblasts. Stem Cells Dev 26 1225 PMID: 28635509
Liu et al (2013) Directed differentiation of forebrain GABA interneurons from human pluripotent stem cells. Nat Protoc 8 1670 PMID: 23928500
Tata et al (2018) Myoepithelial Cells of Submucosal Glands Can Function as Reserve Stem Cells to Regenerate Airways after Injury. Cell Stem Cell 22 668 PMID: 29656943
Levardon et al (2018) Expansion of Airway Basal Cells and Generation of Polarized Epithelium. Bio Protoc 8 PMID: 30009215
Wang et al (2018) The COPII cargo adapter SEC24C is essential for neuronal homeostasis. J Clin Invest 128 3319 PMID: 29939162
Li et al (2018) Fast Generation of Functional Subtype Astrocytes from Human Pluripotent Stem Cells. Stem Cell Reports 11 998 PMID: 30269954
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
Duan et al (2021) An airway organoid-based screen identifies a role for the HIF1α-glycolysis axis in SARS-CoV-2 infection. Cell Rep. 37 109920 PMID: 34731648
Xiong et al (2021) Human Stem Cell-Derived Neurons Repair Circuits and Restore Neural Function Cell Stem Cell 28 112 PMID: 32966778
Frith and Tsakiridis (2019) Efficient Generation of Trunk Neural Crest and Sympathetic Neurons from Human Pluripotent Stem Cells Via a Neuromesodermal Axial Progenitor Intermediate. Curr Protoc Stem Cell Biol 49 e81 PMID: 30688409
Martínez et al (2015) The BMP Pathway Participates in Human Naive CD4+ T Cell Activation and Homeostasis. Cell 10 e0131453 PMID: 26110906
McDonald et al (2015) Myocardin-related transcription factor A regulates conversion of progenitors to beige adipocytes. Arthritis Res Ther 160 105 PMID: 25579684
Varas et al (2015) Blockade of bone morphogenetic protein signaling potentiates the pro-inflammatory phenotype induced by interleukin-17 and tumor necrosis factor-α combination in rheumatoid synoviocytes. Lab Chip 17 192 PMID: 26215036
Du et al (2015) Generation and expansion of highly pure motor neuron progenitors from human pluripotent stem cells. Nat.Commun. 6 6626 PMID: 25806427
Ying et al (2021) Airway basal stem cells generate distinct subpopulations of PNECs. Cell Rep 35 109011 PMID: 33882306
Anestis et al (2021) Generating Enteric Nervous System Progenitors from Human Pluripotent Stem Cells. Curr Protoc 1 e137 PMID: 34102038
Anestis et al (2021) In Vitro Generation of Posterior Motor Neurons from Human Pluripotent Stem Cells. Curr Protoc 1 e244 PMID: 34547185
Viktoriya et al (2021) Autologous transplant therapy alleviates motor and depressive behaviors in parkinsonian monkeys. Nat Med 27 632-639 PMID: 33649496
Jiou et al (2021) C9orf72 regulates energy homeostasis by stabilizing mitochondrial complex I assembly. Cell Metab 33 531-546.e9 PMID: 33545050
Sato et al (2019) Core Transcription Factors Promote Induction of PAX3-Positive Skeletal Muscle Stem Cells. Stem Cell Reports 13 352 PMID: 31353225
Anna et al (2015) Bone morphogenetic protein signaling promotes morphogenesis of blood vessels, wound epidermis, and actinotrichia during fin regeneration in zebrafish. FASEB J 29 4299-312 PMID: 26148971
Li et al (2013) Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments. J Biol Chem 13 1969 PMID: 23563587
Peterson et al (2019) Activating a Reserve Neural Stem Cell Population In Vitro Enables Engraftment and Multipotency after Transplantation. Stem Cell Reports 12 680 PMID: 30930245
Hackland et al (2019) FGF Modulates the Axial Identity of Trunk hPSC-Derived Neural Crest but Not the Cranial-Trunk Decision. Stem Cell Reports 12 920 PMID: 31091435
Bradley E et al (2017) Single-Cell Transcriptomic Analysis of Primary and Metastatic Tumor Ecosystems in Head and Neck Cancer. Cell 171 1611-1624.e24 PMID: 29198524
Ibon et al (2019) Derivation of Neural Stem Cells from Human Parthenogenetic Stem Cells. Methods Mol Biol 1919 43-57 PMID: 30656620
Harikrishna et al (2019) Dual TGFβ/BMP Pathway Inhibition Enables Expansion and Characterization of Multiple Epithelial Cell Types of the Normal and Cancerous Breast. Mol Cancer Res 17 1556-1570 PMID: 30992305
Nadine et al (2019) Endothelial Calcineurin Signaling Restrains Metastatic Outgrowth by Regulating Bmp2. Cell Rep 26 1227-1241.e6 PMID: 30699351
Diane K et al (2018) Astrocyte-enriched feeder layers from cryopreserved cells support differentiation of spontaneously active networks of human iPSC-derived neurons. J Neurosci Methods 294 91-101 PMID: 28746822
Masato et al (2018) Turbulence Activates Platelet Biogenesis to Enable Clinical Scale Ex Vivo Production. Cell 174 636-648.e18 PMID: 30017246
F et al (2022) P97/VCP ATPase inhibitors can rescue p97 mutation-linked motor neuron degeneration. Brain Commun 4 fcac176 PMID: 35865348
Shaochen et al (2022) Isolation and Expansion of Primary Conjunctival Stem Cells (CjSCs) from Human and Rabbit Tissues. Bio Protoc 12 PMID: 36618088
Cheng et al (2022) Genome-wide identification of the genetic basis of amyotrophic lateral sclerosis. Neuron 110 992-1008.e11 PMID: 35045337
Mary Lou et al (2022) A multimodal iPSC platform for cystic fibrosis drug testing. Nat Commun 13 4270 PMID: 35906215
Simon C et al (2022) Engineering rotating apical-out airway organoid for assessing respiratory cilia motility. iScience 25 104730 PMID: 35942088
Ming et al (2022) Recapitulating human cardio-pulmonary co-development using simultaneous multilineage differentiation of pluripotent stem cells. Elife 11 PMID: 35018887
Yan et al (2022) Fast generation of forebrain oligodendrocyte spheroids from human embryonic stem cells by transcription factors. iScience 25 105172 PMID: 36217550
Kalpaj R et al (2022) A Novel Bioreactor for Reconstitution of the Epithelium and Submucosal Glands in Decellularized Ferret Tracheas. Cells 11 PMID: 35326478
Lynch et al (2018) Submucosal Gland Myoepithelial Cells Are Reserve Stem Cells That Can Regenerate Mouse Tracheal Epithelium. Cell Stem Cell 22 653 PMID: 29656941
Mou et al (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell Stem Cell 19 217 PMID: 27320041
Lu et al (2016) Generation of serotonin neurons from human pluripotent stem cells. Nat Biotechnol 34 89 PMID: 26655496
Do you know of a great paper that uses DMH-1 from Tocris? Please let us know.
Reviews for DMH-1
Average Rating: 5 (Based on 3 Reviews.)
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The hiPSCs were maintained with Essential 8 Flex Medium with DMH-1.
By
Anonymous on 02/08/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: ipsc
2 μM
works great for cell line culture.
By
Anonymous on 08/08/2019
Assay Type: In Vitro
Species: Human
I used it grow primary human and mouse airway basal cells
for growing cells.
By
Anonymous on 02/28/2019
Assay Type: In Vitro
Species: Human
I used it grow human airway basal cells
Literature in this Area
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Pathways for DMH-1
