C24 H20 N4 O
|Chemical Name||Quinoline, 4-[6-[4-(1-methylethoxy)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-|
|Solubility (25°C) *||In vitro||DMSO||22 mg/mL warmed (57.82 mM)|
|In vivo||2% DMSO+35% PEG 300+2% Tween 80+ddH2O||2mg/mL|
* <1 mg/ml means slightly soluble or insoluble.
* 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.
|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.|
|In vitro||DMH1 inhibits BMP signaling with IC50 of 100 nM, and selectively inhibits the BMP-induced Smad1/5/8 activation.  DMH1 increases cardiomyocyte progenitors and promotes cardiac differentiation in mouse embryonic stem cells.  In addition, DMH1 as a BMP inhibitor, significantly reduces NSCLC cell growth, migration and invasion. |
|In vivo||DMH1 dorsalizes the embryonic axis without disrupting the angiogenic process in Zebrafish embryos.  In proepicardial explants, DMH1 results in the greatest inhibition of epithelial sheet migration.  DMH1 (5 mg/kg i.p.)attenuates xenograft lung tumor growth in mice bearing A549 xenograft. |
|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 lines||A549 cells|
|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 Models||Mice bearing A549 xenograft.|
|Formulation||12.5% 2-hydroxypropyl-β-cyclodextrin every other day|
Data from [Data independently produced by , , Anticancer Res, 2017, 37(8):4319-4327]
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.
Therapeutic Role of MiR-140-5p for the Treatment of Non-small Cell Lung Cancer. [Flamini V, et al. Anticancer Res, 2017, 37(8):4319-4327]PubMed: 28739724
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