DMH-1

Name: DMH-1
Brand: Tocris Bioscience
SKU: 4126
Rating: 5 (3 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 4126

(3)

Citations (202)

COA / SDS

Selective ALK2 inhibitor

Key Product Details

Description:	Selective ALK2 inhibitor
Chemical Name:	4-[6-[4-(1-Methylethoxy)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline
Purity:	≥98% (HPLC)
Molecular Weight:	380.44

View Full Technical Details for DMH-1

Technical Data
Citations / Reviews (3)

Biological Activity for DMH-1

DMH-1 is a selective inhibitor of bone morphogenic protein (BMP) type-I receptor activin receptor-like kinase 2 (ALK2) receptor (IC₅₀ = 108 nM or 12.6 nM in in vitro kinase assays). DMH-1 exhibits 6- and 19-fold selectivity for ALK-2 over ALK-1 and ALK-3, respectively, and no significant inhibition of AMPK, ALK5, KDR (VEGFR-2) or PDGFRβ receptors. DMH-1 blocks BMP4-induced phosphorylation of Smads 1, 5 and 8 in HEK293 cells. Promotes neurogenesis in human induced pluripotent stem cells (iPSCs) when used in combination with SB 431542 (Cat. No. 1614). DMH-1 suppresses lung cancer cell proliferation, migration, invasion in vitro and reduces tumor growth in a mouse lung cancer xenograft model. DMH-1 inhibits cellular autophagy responses. DMH-1 induces intestinal differentiation in human intestinal organoids (hIOs) derived from human pluripotent stems cells (hPSCs). The compound can also be used in protocols for the chemical reprogramming of somatic cells to iPSCs.

Compound Libraries for DMH-1

DMH-1 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for DMH-1

M. Wt	380.44
Formula	C₂₄H₂₀N₄O
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	1206711-16-1
PubChem ID	50997747
InChi Key	JMIFGARJSWXZSH-UHFFFAOYSA-N
Smiles	CC(C)OC(C=C3)=CC=C3C(C=N2)=CN1C2=C(C4=CC=NC5=C4C=CC=C5)C=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for DMH-1

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	7.61	20

Preparing Stock Solutions for DMH-1

The following data is based on the product molecular weight 380.44.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	13.14 mL	65.71 mL	131.43 mL
1 mM	2.63 mL	13.14 mL	26.29 mL
2 mM	1.31 mL	6.57 mL	13.14 mL
10 mM	0.26 mL	1.31 mL	2.63 mL

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References for DMH-1

References are publications that support the biological activity of the product.

Guan Chemical reprogramming of human somatic cells to pluripotent stem cells. Nature 2022 PMID: 35418683
Sheng DMH1 (4-[6-(4-isopropoxyphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline) inhibits chemotherapeutic drug-induced autophagy. Acta Pharmacol.Sinica 2015 PMID: 26579463
Jung In vitro and in vivo imaging and tracking of intestinal organoids from human induced pluripotent stem cells. FASEB J. 2018 PMID: 28855280
Hao DMH1, a small molecule inhibitor of BMP type i receptors, suppresses growth and invasion of lung cancer. PLoS One 2014 PMID: 24603907
Mohedas Development of an ALK2-biased BMP type I receptor kinase inhibitor. ACS Chem.Biol. 2013 PMID: 23547776
Neely DMH1, a highly selective small molecule BMP inhibitor, promotes neurogenesis of hiPSCs: comparison of PAX6 and SOX1 expression during neural induction. ACS Chem.Neurosci. 2012 PMID: 22860217
Hao In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. ACS Chem.Biol. 2010 PMID: 20020776
Bowman and Zon Swimming into the future of drug discovery: in vivo chemical screens in zebrafish. ACS Chem.Biol. 2010 PMID: 20166761