Home / BMP and Other Activin Receptor Inhibitors / DMH-1

DMH-1

Catalog #: 4126
50 Citations 1 Review Datasheet / COA / SDS
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4126/50
DMH-1 | CAS No. 1206711-16-1 | BMP and Other Activin Receptor Inhibitors
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Description: Selective ALK2 inhibitor

Chemical Name: 4-[6-[4-(1-Methylethoxy)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline

Purity: ≥98%

Product Details
Citations (50)
Supplemental Products
Reviews (1)
Biological Activity Technical Data Background Product Datasheets Calculators

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

M.Wt:
380.44
Formula:
C24H20N4O
Solubility:
Soluble to 20 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
1206711-16-1

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.

Background References

  1. SMAD1/5 mediates bone morphogenetic protein 2-induced up-regulation of BAMBI expression in human granulosa-lutein cells
    L Bai, HM Chang, JC Cheng, C Klausen, G Chu, PCK Leung, G Yang
    Cell. Signal., 2017;37(0):52-61.
  2. Optimal effector functions in human natural killer cells rely upon autocrine bone morphogenetic protein signaling.
    Robson N, Hidalgo L, McAlpine T, Wei H, Martinez V, Entrena A, Melen G, MacDonald A, Phythian-Adams A, Sacedon R, Maraskovsky E, Cebon J, Ramirez M, Vicente A, Varas A
    Cancer Res, 2014;74(18):5019-31.
  3. Bone morphogenetic protein 2 promotes human trophoblast cell invasion by upregulating N-cadherin via non-canonical SMAD2/3 signaling
    HJ Zhao, C Klausen, Y Li, H Zhu, YL Wang, PCK Leung
    Cell Death Dis, 2018;9(2):174.
  4. Loss of ACVRIB leads to increased squamous cell carcinoma aggressiveness through alterations in cell-cell and cell-matrix adhesion proteins
    HA Loomans, SA Arnold, K Hebron, CJ Taylor, A Zijlstra, CD Andl
    Am J Cancer Res, 2017;7(12):2422-2437.
  5. Bone morphogenetic protein 2 regulates cell-cell communication by down-regulating connexin43 expression in luteinized human granulosa cells
    Yan-Ting Wu
    Mol. Hum. Reprod, 2016;0(0):.
  6. Activin-A enhances mTOR signaling to promote aberrant chondrogenesis in fibrodysplasia ossificans progressiva
    K Hino, K Horigome, M Nishio, S Komura, S Nagata, C Zhao, Y Jin, K Kawakami, Y Yamada, A Ohta, J Toguchida, M Ikeya
    J. Clin. Invest., 2017;0(0):.
  7. The COPII cargo adapter SEC24C is essential for neuronal homeostasis
    B Wang, JH Joo, R Mount, BJW Teubner, A Krenzer, AL Ward, VP Ichhaporia, EJ Adams, R Khoriaty, ST Peters, SM Pruett-Mil, SS Zakharenko, D Ginsburg, M Kundu
    J. Clin. Invest., 2018;0(0):.
  8. Bone morphogenetic protein 2 increases lysyl oxidase activity via up-regulation of snail in human granulosa-lutein cells
    L Bai, HM Chang, YM Zhu, PCK Leung
    Cell. Signal., 2018;53(0):201-211.
  9. Development of an ALK2-biased BMP type I receptor kinase inhibitor.
    Mohedas et al.
    ACS Chem.Biol., 2013;8:1291
  10. 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
  11. Swimming into the future of drug discovery: in vivo chemical screens in zebrafish.
    Bowman and Zon
    ACS Chem.Biol., 2010;5:159
  12. In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.
    Hao et al.
    ACS Chem.Biol., 2010;5:245
  13. Human iPSC-Derived Neural Crest Stem Cells Exhibit Low Immunogenicity
    VJ Mehler, CJ Burns, H Stauss, RJ Francis, ML Moore
    Mol Ther Methods Clin Dev, 2020;16(0):161-171.
  14. In Vitro CRISPR/Cas9-Directed Gene Editing to Model LRRK2 G2019S Parkinson's Disease in Common Marmosets
    SC Vermilyea, A Babinski, N Tran, S To, S Guthrie, JH Kluss, JK Schmidt, GJ Wiepz, MG Meyer, ME Murphy, MR Cookson, ME Emborg, TG Golos
    Sci Rep, 2020;10(1):3447.

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Citations for DMH-1

The citations listed below are publications that use Tocris products. Selected citations for DMH-1 include:

50 Citations: Showing 1 - 10

  1. Axon guidance genes modulate neurotoxicity of ALS-associated UBQLN2.
    Authors: Mark Et al.
    Elife  2023;12
  2. P97/VCP ATPase inhibitors can rescue p97 mutation-linked motor neuron degeneration.
    Authors: F Et al.
    Brain Commun  2022;4:fcac176
  3. Fast generation of forebrain oligodendrocyte spheroids from human embryonic stem cells by transcription factors.
    Authors: Yan Et al.
    iScience  2022;25:105172
  4. Engineering rotating apical-out airway organoid for assessing respiratory cilia motility.
    Authors: Simon C Et al.
    iScience  2022;25:104730
  5. A multimodal iPSC platform for cystic fibrosis drug testing.
    Authors: Mary Lou Et al.
    Nat Commun  2022;13:4270
  6. Isolation and Expansion of Primary Conjunctival Stem Cells (CjSCs) from Human and Rabbit Tissues.
    Authors: Shaochen Et al.
    Bio Protoc  2022;12
  7. Genome-wide identification of the genetic basis of amyotrophic lateral sclerosis.
    Authors: Cheng Et al.
    Neuron  2022;110:992-1008.e11
  8. A Novel Bioreactor for Reconstitution of the Epithelium and Submucosal Glands in Decellularized Ferret Tracheas.
    Authors: Kalpaj R Et al.
    Cells  2022;11
  9. Recapitulating human cardio-pulmonary co-development using simultaneous multilineage differentiation of pluripotent stem cells.
    Authors: Ming Et al.
    Elife  2022;11
  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
  11. Airway basal stem cells generate distinct subpopulations of PNECs.
    Authors: Ying Et al.
    Cell Rep  2021;35:109011
  12. C9orf72 regulates energy homeostasis by stabilizing mitochondrial complex I assembly.
    Authors: Jiou Et al.
    Cell Metab  2021;33:531-546.e9
  13. Human Stem Cell-Derived Neurons Repair Circuits and Restore Neural Function
    Authors: Xiong Et al.
    Cell Stem Cell  2021;28:112
  14. Autologous transplant therapy alleviates motor and depressive behaviors in parkinsonian monkeys.
    Authors: Viktoriya Et al.
    Nat Med  2021;27:632-639
  15. In Vitro Generation of Posterior Motor Neurons from Human Pluripotent Stem Cells.
    Authors: Anestis Et al.
    Curr Protoc  2021;1:e244
  16. Generating Enteric Nervous System Progenitors from Human Pluripotent Stem Cells.
    Authors: Anestis Et al.
    Curr Protoc  2021;1:e137
  17. 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.
    Authors: Lee J Et al.
    Acta Neuropathol Commun  2020;8:7
  18. Human Bocavirus 1 Infection of Well-Differentiated Human Airway Epithelium.
    Authors: Jianming Et al.
    Curr Protoc Microbiol  2020;58:e107
  19. The omentum of obese girls harbors small adipocytes and browning transcripts.
    Authors: Gerald I Et al.
    JCI Insight  2020;5
  20. BMP signaling plays a role in anterior-neural/head development, but not organizer activity, in the gastropod Crepidula fornicata.
    Authors: Kimberly J Et al.
    Dev Biol  2020;463:135-157
  21. Human Motor Neurons With SOD1-G93A Mutation Generated From CRISPR/Cas9 Gene-Edited iPSCs Develop Pathological Features of Amyotrophic Lateral Sclerosis.
    Authors: Lee J Et al.
    Front Cell Neurosci  2020;14:604171
  22. Generation and trapping of a mesoderm biased state of human pluripotency.
    Authors: Jason Et al.
    Nat Commun  2020;11:4989
  23. Multiplatform genomic profiling and magnetic resonance imaging identify mechanisms underlying intratumor heterogeneity in meningioma.
    Authors: Erik M Et al.
    Nat Commun  2020;11:4803
  24. In Vitro CRISPR/Cas9-Directed Gene Editing to Model LRRK2 G2019S Parkinson's Disease in Common Marmosets.
    Authors: Thaddeus G Et al.
    Sci Rep  2020;10:3447
  25. 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
  26. Endothelial Calcineurin Signaling Restrains Metastatic Outgrowth by Regulating Bmp2.
    Authors: Nadine Et al.
    Cell Rep  2019;26:1227-1241.e6
  27. Derivation of Neural Stem Cells from Human Parthenogenetic Stem Cells.
    Authors: Ibon Et al.
    Methods Mol Biol  2019;1919:43-57
  28. Dual TGFβ/BMP Pathway Inhibition Enables Expansion and Characterization of Multiple Epithelial Cell Types of the Normal and Cancerous Breast.
    Authors: Harikrishna Et al.
    Mol Cancer Res  2019;17:1556-1570
  29. Core Transcription Factors Promote Induction of PAX3-Positive Skeletal Muscle Stem Cells.
    Authors: Sato Et al.
    Stem Cell Reports  2019;13:352
  30. 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
  31. 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
  32. 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
  33. Expansion of Airway Basal Cells and Generation of Polarized Epithelium.
    Authors: Levardon Et al.
    Bio Protoc  2018;8
  34. Astrocyte-enriched feeder layers from cryopreserved cells support differentiation of spontaneously active networks of human iPSC-derived neurons.
    Authors: Diane K Et al.
    J Neurosci Methods  2018;294:91-101
  35. 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
  36. Submucosal Gland Myoepithelial Cells Are Reserve Stem Cells That Can Regenerate Mouse Tracheal Epithelium.
    Authors: Lynch Et al.
    Cell Stem Cell  2018;22:653
  37. Turbulence Activates Platelet Biogenesis to Enable Clinical Scale Ex Vivo Production.
    Authors: Masato Et al.
    Cell  2018;174:636-648.e18
  38. The COPII cargo adapter SEC24C is essential for neuronal homeostasis.
    Authors: Wang Et al.
    J Clin Invest  2018;128:3319
  39. Fast Generation of Functional Subtype Astrocytes from Human Pluripotent Stem Cells.
    Authors: Li Et al.
    Stem Cell Reports  2018;11:998
  40. Induced Pluripotent Stem Cell-Derived Dopaminergic Neurons from Adult Common Marmoset Fibroblasts.
    Authors: Vermilyea Et al.
    Stem Cells Dev  2017;26:1225
  41. Single-Cell Transcriptomic Analysis of Primary and Metastatic Tumor Ecosystems in Head and Neck Cancer.
    Authors: Bradley E Et al.
    Cell  2017;171:1611-1624.e24
  42. Generation of serotonin neurons from human pluripotent stem cells.
    Authors: Lu Et al.
    Nat Biotechnol  2016;34:89
  43. Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
    Authors: Mou Et al.
    Cell Stem Cell  2016;19:217
  44. Generation and expansion of highly pure motor neuron progenitors from human pluripotent stem cells.
    Authors: Du Et al.
    Nat.Commun.  2015;6:6626
  45. Bone morphogenetic protein signaling promotes morphogenesis of blood vessels, wound epidermis, and actinotrichia during fin regeneration in zebrafish.
    Authors: Anna Et al.
    FASEB J  2015;29:4299-312
  46. 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
  47. Myocardin-related transcription factor A regulates conversion of progenitors to beige adipocytes.
    Authors: McDonald Et al.
    Arthritis Res Ther  2015;160:105
  48. The BMP Pathway Participates in Human Naive CD4+ T Cell Activation and Homeostasis.
    Authors: Martínez Et al.
    Cell  2015;10:e0131453
  49. Directed differentiation of forebrain GABA interneurons from human pluripotent stem cells.
    Authors: Liu Et al.
    Nat Protoc  2013;8:1670
  50. 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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Somatic cells to iPS cells
By Anonymous on 11/08/2023
Species: Human

Used on somatic cells to iPSCs cells. We use these ipsc cells to differentiate into neural cells. Batch number: 4A/256409

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