DMH1

Catalog No.S7146 Batch:S714601

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Technical Data

Formula

C24 H20 N4 O
Molecular Weight 380.44 CAS No. 1206711-16-1
Solubility (25°C)* In vitro DMSO 32 mg/mL (84.11 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. DMH1 inhibits autophagy.
Targets
ALK2 [1]
(Cell-free assay)
107.9 nM
In vitro DMH1 inhibits BMP signaling with IC50 of 100 nM, and selectively inhibits the BMP-induced Smad1/5/8 activation. [1] DMH1 increases cardiomyocyte progenitors and promotes cardiac differentiation in mouse embryonic stem cells. [3] In addition, DMH1 as a BMP inhibitor, significantly reduces NSCLC cell growth, migration and invasion. [4]
In vivo DMH1 dorsalizes the embryonic axis without disrupting the angiogenic process in Zebrafish embryos. [1] In proepicardial explants, DMH1 results in the greatest inhibition of epithelial sheet migration. [2] DMH1 (5 mg/kg i.p.)attenuates xenograft lung tumor growth in mice bearing A549 xenograft. [4]

Protocol (from reference)

Kinase Assay:[1]
  • Kinase assay

    All kinase assays are conducted by Reaction Biology Corp. In brief, compounds are tested at 10 concentrations by 3-fold serial dilutions starting at 30 μM, using nonspecific kinase inhibitor staurosporine as control. In vitro kinase reactions are carried out in the presence of 10 μM (33P)γATP. Five kinases tested are the human BMP type-I receptor activin receptor-like kinase 2 (ALK-2/ACVR1), the human TGFβ type-I receptor activin receptor-like kinase 5 (Alk5/TGFβR1), the human VEGF type-II receptor (KDR/Flk-1/VEGFR2), the human AMP-activated protein kinase (AMPK/A1/B1/G1) and the human platelet-derived growth factor receptor-β (PDGFRβ).
Cell Assay:[4]
  • Cell lines

    A549 cells

  • Concentrations

    ~5 μM

  • Incubation Time

    48-96 hours

  • Method

    About 10,000 A549 cells per well are seeded in 96-well plates and incubated for overnight. The culture medium is then changed to fresh medium containing DMSO or DMH1 at various concentrations. The cells are then incubated for 48 hours and 96 hours before treatment termination by replacing the medium with 100 μL of 10% trichloroacetic acid in 1× PBS, followed by incubation at 4°C for at least 1 hour. Subsequently, the plates are washed with water and air dried. The plates are stained with 50 μL 0.4% sulphorhodamine assay in 1% acetic acid for 30 minutes at room temperature. Unbound dye is washed off with 1% acetic acid. After air drying and solubilization of the protein-bound dye in 10 mM Tris solution, absorbance is read in a microplate reader at 565 nm.
Animal Study:[4]
  • Animal Models

    Mice bearing A549 xenograft.

  • Dosages

    ~5 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Anticancer Res, 2017, 37(8):4319-4327]

Selleck's DMH1 has been cited by 46 publications

A TBK1 variant causes autophagolysosomal and motoneuron pathology without neuroinflammation in mice [ J Exp Med, 2024, 221(5)e20221190] PubMed: 38517332
The MORC2 p.S87L mutation reduces proliferation of pluripotent stem cells derived from a patient with the spinal muscular atrophy-like phenotype by inhibiting proliferation-related signaling pathways [ Neural Regen Res, 2024, 19(1):205-211] PubMed: 37488868
Homozygous ALS-linked mutations in TARDBP/TDP-43 lead to hypoactivity and synaptic abnormalities in human iPSC-derived motor neurons [ iScience, 2024, 27(3):109166] PubMed: 38433895
Bmp8a deletion leads to obesity through regulation of lipid metabolism and adipocyte differentiation [ Commun Biol, 2023, 6(1):824] PubMed: 37553521
BMP8B Activates Both SMAD2/3 and NF-κB Signals to Inhibit the Differentiation of 3T3-L1 Preadipocytes into Mature Adipocytes [ Nutrients, 2023, 16(1)64] PubMed: 38201894
Bmp4 in Zebrafish Enhances Antiviral Innate Immunity through p38 MAPK -Mitogen-Activated Protein Kinases) Pathway [ Int J Mol Sci, 2023, 24(19)14444] PubMed: 37833891
Reduced C9orf72 expression exacerbates polyGR toxicity in patient iPSC-derived motor neurons and a Type I protein arginine methyltransferase inhibitor reduces that toxicity [ Front Cell Neurosci, 2023, 17:1134090] PubMed: 37138766
BMP signaling inhibition overcomes chemoresistance of prostate cancer [ Am J Cancer Res, 2023, ] PubMed: 37818054
Comparing Cytology Brushes for Optimal Human Nasal Epithelial Cell Collection: Implications for Airway Disease Diagnosis and Research [ J Pers Med, 2023, 13(5)864] PubMed: 37241034
Notch signaling inactivation by small molecule γ-secretase inhibitors restores the multiciliated cell population in the airway epithelium [ Am J Physiol Lung Cell Mol Physiol, 2023, 324(6):L771-L782] PubMed: 37039381

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.