Chemical Name: 4-[6-[4-(1-Methylethoxy)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline
Biological ActivityDMH-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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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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
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
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
Human Stem Cell-Derived Neurons Repair Circuits and Restore Neural Function
Authors: Xiong Et al.
Cell Stem Cell 2021;28:112
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
Core Transcription Factors Promote Induction of PAX3-Positive Skeletal Muscle Stem Cells.
Authors: Sato Et al.
Stem Cell Reports 2019;13:352
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
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
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
Expansion of Airway Basal Cells and Generation of Polarized Epithelium.
Authors: Levardon Et al.
Bio Protoc 2018;8
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
Submucosal Gland Myoepithelial Cells Are Reserve Stem Cells That Can Regenerate Mouse Tracheal Epithelium.
Authors: Lynch Et al.
Cell Stem Cell 2018;22:653
The COPII cargo adapter SEC24C is essential for neuronal homeostasis.
Authors: Wang Et al.
J Clin Invest 2018;128:3319
Fast Generation of Functional Subtype Astrocytes from Human Pluripotent Stem Cells.
Authors: Li Et al.
Stem Cell Reports 2018;11:998
Induced Pluripotent Stem Cell-Derived Dopaminergic Neurons from Adult Common Marmoset Fibroblasts.
Authors: Vermilyea Et al.
Stem Cells Dev 2017;26:1225
Generation of serotonin neurons from human pluripotent stem cells.
Authors: Lu Et al.
Nat Biotechnol 2016;34:89
Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
Authors: Mou Et al.
Cell Stem Cell 2016;19:217
Generation and expansion of highly pure motor neuron progenitors from human pluripotent stem cells.
Authors: Du Et al.
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
Myocardin-related transcription factor A regulates conversion of progenitors to beige adipocytes.
Authors: McDonald Et al.
Arthritis Res Ther 2015;160:105
The BMP Pathway Participates in Human Naive CD4+ T Cell Activation and Homeostasis.
Authors: Martínez Et al.
Directed differentiation of forebrain GABA interneurons from human pluripotent stem cells.
Authors: Liu Et al.
Nat Protoc 2013;8:1670
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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