DMH1

For research use only.

Catalog No.S7146

10 publications

DMH1 Chemical Structure

Molecular Weight(MW): 380.44

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.

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Selleck's DMH1 has been cited by 10 publications

1 Customer Review

  • The combined treatment with miR-140-5p mimics and some common chemotherapeutics did not have any effect on the SK-MES1 cell line, whereas miR-140-5p and DMH1 and cisplatin decreased the proliferation of the A549 cells. Data are presented as mean±SEM of three individual experiments undertaken in triplicate. t-Test was used to assess significance with *p<0.05.

    Anticancer Res, 2017, 37(8):4319-4327. DMH1 purchased from Selleck.

Purity & Quality Control

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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.
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVECs NXfYSWxPTnWwY4Tpc44h[XO|YYm= NGPucVU1NjVizszN NVrVW4R5OiCq NH3UT4x{cW23bIThcoVwfXNic4TpcZVt[XSrb36gc4YhSk2SRWKgZY5lKEKPUESgeI9o\XSqZYKge4l1cCCGTVixJJBz\X[nboTl[EBifWevZX70ZZRqd25ib3[gUmlETCCjbnSgTGVUOSCxbjD0bIUheHKxdHXpckBt\X[nbB?= M3TDZlI6PDd|OUm3
HeLa M{HwfmZ2dmO2aX;uJIF{e2G7 M3ftUFUh|ryvb3yvUEBidmRiMUCg{txud2xxTB?= NV2xfWR[OjUEoHi= NHP4VJlFVUhzIHnubIljcXSnZDDDSGRRNWmwZIXj[YQh[XW2b4DoZYd6KGmwIFjlUIEh[2WubIOu NFS4e5IzPjV5OUS2Ny=>
MCF-7 M1rze2Z2dmO2aX;uJIF{e2G7 MXe1JO69dW:uL1ygZY5lKDFyIN88cY9tN0x? M2e0bFI1yqCq MVTjc41xdGW2ZXz5JIFjd2yrc3jl[EB1cGVidHHtc5hq\mWwLXnu[JVk\WRiaX7jdoVie2Vib3[gZZV1d3CqYXf5JJJme3CxboPld{BqdiCPQ1[tO{Bk\Wyucx?= NYLLR4ZnOjZ3N{m0OlM>
OVCAR3 NELGUYNHfW6ldHnvckBie3OjeR?= NXPoTWlWOjBizszN NIXKOGozPMLiaB?= MnX0doVlfWOnIITo[UBk[W6xbnnjZYwheGixc4Doc5J6dGG2aX;uJI9nKFOvYXTzJFEtPSCjbnSgPS=> NWq1NmduOjZ{M{WxN|k>
OVCAR8 NX3sWnJqTnWwY4Tpc44h[XO|YYm= NXuwUmJzOjBizszN MnrvNlTDqGh? M1\x[ZJm\HWlZTD0bIUh[2Gwb37pZ4FtKHCqb4PwbI9zgWyjdHnvckBw\iCVbXHkd{AyNDViYX7kJFk> M4rDOFI3OjN3MUO5
SKOV3 MmXxSpVv[3Srb36gZZN{[Xl? MYeyNEDPxE1? NXPYTYZWOjUEoHi= NXnvWXJOemWmdXPlJJRp\SClYX7vcolk[WxicHjvd5Bpd3K7bHH0bY9vKG:oIGPtZYR{KDFuNTDhcoQhQQ>? M3Gx[lI3OjN3MUO5
A549 Mo\OSpVv[3Srb36gZZN{[Xl? MmjNN{BidmRiNTFCuW0> NH[4SXAzPMLiaB?= MonySG1JOSC2cnXheI1mdnRiZX\m[YN1cX[nbImgZoxw[2unZDDTcYFlKDFxNT:4JJBpd3OyaH;yfYxifGmxbjDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MX:yOFYxOzlyNx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Integrin β1 / p-Smad / Smad1 / p-AKT / AKT ; 

PubMed: 26337467     


MTT cells were treated with DMH1 (3 μM or 5 μM) or with DMSO vehicle for 24 h. Proteins were then collected and probed for the expression of integrin β1, P-Smad1/5/8, Smad1, P-AKT and AKT. α-Tubulin was used as a loading control. 

26337467
Growth inhibition assay
Cell proliferation; 

PubMed: 26337467     


MTT cells were treated with DMH1 (3 μM or 5 μM) or with DMSO vehicle. Proliferation was assessed at the indicated times by the WST-1 assay. The experiments were performed two times with six technical replicates each, and are expressed as the mean ± SD. The values are normalized against those of DMSO-treated cells set to 100%. ***, P < 0.001. 

26337467
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

Kinase Assay:[1]
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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:[4]
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  • 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.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: Mice bearing A549 xenograft.
  • Dosages: ~5 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 22 mg/mL warmed (57.82 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+35% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
2mg/mL

* 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.

Chemical Information

Molecular Weight 380.44
Formula

C24 H20 N4 O

CAS No. 1206711-16-1
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)OC1=CC=C(C=C1)C2=C[N]3N=CC(=C3N=C2)C4=CC=NC5=C4C=CC=C5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Dilution Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID