DMH-1
Chemical Name: 4-[6-[4-(1-Methylethoxy)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline
Purity: ≥98%
Biological Activity
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.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.
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Background References
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Development of an ALK2-biased BMP type I receptor kinase inhibitor.
Mohedas et al.
ACS Chem.Biol., 2013;8:1291 -
DMH1, a highly selective small molecule BMP inhibitor, promotes neurogenesis of hiPSCs: comparison of PAX6 and SOX1 expression during neural induction.
Neely et al.
ACS Chem.Neurosci., 2012;3:482 -
Swimming into the future of drug discovery: in vivo chemical screens in zebrafish.
Bowman and Zon
ACS Chem.Biol., 2010;5:159 -
In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.
Hao et al.
ACS Chem.Biol., 2010;5:245
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Citations for DMH-1
The citations listed below are publications that use Tocris products. Selected citations for DMH-1 include:
21 Citations: Showing 1 - 10
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An airway organoid-based screen identifies a role for the HIF1α-glycolysis axis in SARS-CoV-2 infection.
Authors: Duan Et al.
Cell Rep. 2021;37:109920
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Human Stem Cell-Derived Neurons Repair Circuits and Restore Neural Function
Authors: Xiong Et al.
Cell Stem Cell 2021;28:112
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Efficient Generation of Trunk Neural Crest and Sympathetic Neurons from Human Pluripotent Stem Cells Via a Neuromesodermal Axial Progenitor Intermediate.
Authors: Frith and Tsakiridis
Curr Protoc Stem Cell Biol 2019;49:e81
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Core Transcription Factors Promote Induction of PAX3-Positive Skeletal Muscle Stem Cells.
Authors: Sato Et al.
Stem Cell Reports 2019;13:352
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FGF Modulates the Axial Identity of Trunk hPSC-Derived Neural Crest but Not the Cranial-Trunk Decision.
Authors: Hackland Et al.
Stem Cell Reports 2019;12:920
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Activating a Reserve Neural Stem Cell Population In Vitro Enables Engraftment and Multipotency after Transplantation.
Authors: Peterson Et al.
Stem Cell Reports 2019;12:680
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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
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Expansion of Airway Basal Cells and Generation of Polarized Epithelium.
Authors: Levardon Et al.
Bio Protoc 2018;8
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Myoepithelial Cells of Submucosal Glands Can Function as Reserve Stem Cells to Regenerate Airways after Injury.
Authors: Tata Et al.
Cell Stem Cell 2018;22:668
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Submucosal Gland Myoepithelial Cells Are Reserve Stem Cells That Can Regenerate Mouse Tracheal Epithelium.
Authors: Lynch Et al.
Cell Stem Cell 2018;22:653
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The COPII cargo adapter SEC24C is essential for neuronal homeostasis.
Authors: Wang Et al.
J Clin Invest 2018;128:3319
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Fast Generation of Functional Subtype Astrocytes from Human Pluripotent Stem Cells.
Authors: Li Et al.
Stem Cell Reports 2018;11:998
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Induced Pluripotent Stem Cell-Derived Dopaminergic Neurons from Adult Common Marmoset Fibroblasts.
Authors: Vermilyea Et al.
Stem Cells Dev 2017;26:1225
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Generation of serotonin neurons from human pluripotent stem cells.
Authors: Lu Et al.
Nat Biotechnol 2016;34:89
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Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
Authors: Mou Et al.
Cell Stem Cell 2016;19:217
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Generation and expansion of highly pure motor neuron progenitors from human pluripotent stem cells.
Authors: Du Et al.
Nat.Commun. 2015;6:6626
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Blockade of bone morphogenetic protein signaling potentiates the pro-inflammatory phenotype induced by interleukin-17 and tumor necrosis factor-α combination in rheumatoid synoviocytes.
Authors: Varas Et al.
Lab Chip 2015;17:192
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Myocardin-related transcription factor A regulates conversion of progenitors to beige adipocytes.
Authors: McDonald Et al.
Arthritis Res Ther 2015;160:105
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The BMP Pathway Participates in Human Naive CD4+ T Cell Activation and Homeostasis.
Authors: Martínez Et al.
Cell 2015;10:e0131453
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Directed differentiation of forebrain GABA interneurons from human pluripotent stem cells.
Authors: Liu Et al.
Nat Protoc 2013;8:1670
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Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments.
Authors: Li Et al.
J Biol Chem 2013;13:1969
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