DMH1

Catalog No.S7146

For research use only.

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

CAS No. 1206711-16-1

Selleck's DMH1 has been cited by 25 publications

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. 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVECs MX7GeY5kfGmxbjDhd5NigQ>? M4TXdlQvPSEQvF2= NGDGTIgzKGh? M2DkW5NqdXWudHHu[Y92eyC|dHnteYxifGmxbjDv[kBDVVCHUjDhcoQhSk2SNDD0c4dmfGincjD3bZRpKESPSEGgdJJmfmWwdHXkJIF2\22nboTheIlwdiCxZjDOTWNFKGGwZDDISXMyKG:wIITo[UBxem:2ZXnuJIxmfmWu M4K1eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEezPVk4Lz5{OUS3N|k6PzxxYU6=
HeLa NIr4XVJHfW6ldHnvckBie3OjeR?= NFu0XZI2KM7:bX;sM2wh[W6mIEGwJO69dW:uL1y= MnzLNlTDqGh? MXLEUWgyKGmwaHnibZRm\CCFRFTQMYlv\HWlZXSgZZV1d3CqYXf5JIlvKEinTHGgZ4VtdHNw NXzudFhKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1O|k1PjNpPkK2OVc6PDZ|PD;hQi=>
MCF-7 NFP0cmVHfW6ldHnvckBie3OjeR?= M1O2cVUh|ryvb3yvUEBidmRiMUCg{txud2xxTB?= M4Xsd|I1yqCq NH;FTpJkd22ybHX0[Yx6KGGkb3zpd4hm\CC2aHWgeIFud3irZnXuMYlv\HWlZXSgbY5kemWjc3Wgc4Yh[XW2b4DoZYd6KHKnc4DvcpNmeyCrbjDNR2YuPyClZXzsdy=> M1\DRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUe5OFY{Lz5{NkW3PVQ3OzxxYU6=
OVCAR3 NYL4SoZWTnWwY4Tpc44h[XO|YYm= MkTCNlAh|ryP NWf3N5FwOjUEoHi= Mnr1doVlfWOnIITo[UBk[W6xbnnjZYwheGixc4Doc5J6dGG2aX;uJI9nKFOvYXTzJFEtPSCjbnSgPS=> NYfqdnpvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yN|UyOzlpPkK2NlM2OTN7PD;hQi=>
OVCAR8 MVrGeY5kfGmxbjDhd5NigQ>? MlXkNlAh|ryP MXyyOOKhcA>? M3\rSpJm\HWlZTD0bIUh[2Gwb37pZ4FtKHCqb4PwbI9zgWyjdHnvckBw\iCVbXHkd{AyNDViYX7kJFk> M4T4dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkO1NVM6Lz5{NkKzOVE{QTxxYU6=
SKOV3 NIfRSm9HfW6ldHnvckBie3OjeR?= NVP3V5ppOjBizszN NXrjUXdKOjUEoHi= NGTnXnRz\WS3Y3WgeIhmKGOjbn;ubYNidCCyaH;zdIhwenmuYYTpc44hd2ZiU33h[JMhOSx3IHHu[EA6 MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ|NUGzPUc,OjZ{M{WxN|k9N2F-
A549 MX\GeY5kfGmxbjDhd5NigQ>? Mn23N{BidmRiNTFCuW0> Mk\XNlTDqGh? NFfObJhFVUhzIITy[YF1dWWwdDDl[oZm[3SrdnXsfUBjdG:la3XkJHNu[WRiMT:1M|gheGixc4Doc5J6dGG2aX;uJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZyM{mwO{c,OjR4MEO5NFc9N2F-
Assay
Methods Test Index PMID
Western blot Integrin β1 / p-Smad / Smad1 / p-AKT / AKT 26337467
Growth inhibition assay Cell proliferation 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 (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 Research:[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 Research:[4]
  • Animal Models: Mice bearing A549 xenograft.
  • Dosages: ~5 mg/kg
  • Administration: i.p.

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):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.

0.75mg/mL

Chemical Information

Molecular Weight 380.44
Formula

C24 H20 N4 O

CAS No. 1206711-16-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)OC1=CC=C(C=C1)C2=CN3C(=C(C=N3)C4=CC=NC5=CC=CC=C45)N=C2

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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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