Home TGF-beta/Smad TGF-beta/Smad inhibitor - Autophagy inhibitor DMH1 For research use only.

DMH1

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.

DMH1 Chemical Structure

DMH1 Chemical Structure

CAS No. 1206711-16-1

Purity & Quality Control

DMH1 Related Products

Signaling Pathway

TGF-beta/Smad Signaling Pathways

TGF-beta/Smad Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 Function assay 3 and 5 µM 24 h DMH1 treatment effectively blocked Smad 1/5/8 phosphorylation in a dose dependent manner 24603907
SKOV3 Function assay 20 μM 24 h reduce the canonical phosphorylation of Smads 1,5 and 9 26235139
OVCAR8 Function assay 20 μM 24 h reduce the canonical phosphorylation of Smads 1,5 and 9 26235139
OVCAR3 Function assay 20 μM 24 h reduce the canonical phosphorylation of Smads 1,5 and 9 26235139
MCF-7 Function assay 5 μmol/L and 10 μmol/L 24 h completely abolished the increase of autophagy responses in MCF-7 cells 26579463
HeLa Function assay 5 μmol/L and 10 μmol/L 24 h DMH1 inhibited CDDP-induced autophagy in HeLa cells. 26579463
HUVECs Function assay 4.5 μM 2 h simultaneous stimulation of BMPER and BMP4 together with DMH1 prevented augmentation of NICD and HES1 on the protein level 29473997
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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
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]
Kinase Assay 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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Integrin β1 / p-Smad / Smad1 / p-AKT / AKT 26337467
Growth inhibition assay Cell proliferation 26337467
In Vivo
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]
Animal Research Animal Models Mice bearing A549 xenograft.
Dosages ~5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 380.44 Formula

C24 H20 N4 O
CAS No. 1206711-16-1 SDF Download DMH1 SDF
Smiles CC(C)OC1=CC=C(C=C1)C2=CN3C(=C(C=N3)C4=CC=NC5=CC=CC=C45)N=C2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 25 mg/mL ( (65.71 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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