Name: DMH1
Brand: Selleck Chemicals
SKU: S7146
Availability: InStock
Rating: 5 (61 reviews)

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Quality Control

Batch: Purity: 99.92%

99.92

Related Targets	PKC ROCK Bcr-Abl
Other TGF-beta/Smad Inhibitors	SB431542 RepSox (E-616452) Vactosertib (TEW-7197) LDN-193189 A-83-01 LDN-193189 Dihydrochloride Galunisertib (LY2157299) SRI-011381 (C381) LY2109761 SIS3 Hydrochloride

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 25 mg/mL (65.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.750mg/ml (1.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 35%PEG300 2 2%Tween80 3 61%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.300mg/ml (0.79mM)	Taking the 1 mL working solution as an example, add 20 μL of 15 mg/ml clarified DMSO stock solution to 350 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 610 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	380.44	Formula	C₂₄ H₂₀ N₄ O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1206711-16-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)OC1=CC=C(C=C1)C2=CN3C(=C(C=N3)C4=CC=NC5=CC=CC=C45)N=C2

Mechanism of Action

Targets/IC₅₀/Ki	ALK2 (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. This compound increases cardiomyocyte progenitors and promotes cardiac differentiation in mouse embryonic stem cells. In addition, as a BMP inhibitor, it significantly reduces NSCLC cell growth, migration and invasion.
Kinase Assay	Kinase assay
Kinase Assay	All kinase assays are conducted by Reaction Biology Corp. In brief, this compound is 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).
In vivo	DMH1 dorsalizes the embryonic axis without disrupting the angiogenic process in Zebrafish embryos. In proepicardial explants, this compound results in the greatest inhibition of epithelial sheet migration. This chemical (5 mg/kg i.p.) attenuates xenograft lung tumor growth in mice bearing A549 xenograft.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20020776/ [2] https://pubmed.ncbi.nlm.nih.gov/21740033/ [3] https://pubmed.ncbi.nlm.nih.gov/22848549/ [4] https://pubmed.ncbi.nlm.nih.gov/24603907/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Integrin β1 / p-Smad / Smad1 / p-AKT / AKT		26337467
Growth inhibition assay	Cell proliferation		26337467

Tech Support

Handling Instructions

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DMH1 TGF-beta/Smad inhibitor

Chemical Structure

Molecular Weight: 380.44