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DMH1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
DMH1图片
CAS NO:1206711-16-1
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)380.44
FormulaC24H20N4O
CAS No.1206711-16-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 22 mg/mL (57.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other infoChemical Name: 4-(6-(4-isopropoxyphenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline

SMILES Code: CC(OC1=CC=C(C2=CN3C(N=C2)=C(C4=CC=NC5=CC=CC=C45)C=N3)C=C1)C

Exact Mass: 380.16371

SynonymsDMH 1; DMH-1; DMH1;
实验参考方法
In Vitro

In vitro activity: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.


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 Assay: 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.

In VivoDMH1 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.
Animal modelMice bearing A549 xenograft.
Formulation & DosageDissolved in 12.5% 2-hydroxypropyl-β-cyclodextrin; 5 mg/kg; i.p. injection
References

ACS Chem Biol. 2010 Feb 19;5(2):245-53; ACS Chem Biol. 2011 Sep 16;6(9):952-61.