DMH1 是一种选择性BMP抑制剂，对 ALK1、ALK2、ALK3和ALK6的IC50值分别为 27、107.9、<5和 47.6 nM。

DMH-1 is a potent and selective BMP inhibitor.

5 mg/kg i.p. DMH1减弱携带A549异种移植物的小鼠中的异种移植肺肿瘤生长.DMH1在前心外膜移植组织中,引起对上皮细胞层迁移的最大抑制.

DMH1作为一种BMP抑制剂,可显著降低NSCLC细胞生长,迁移和侵袭。DMH1抑制BMP信号,IC50 为100 nM,并选择性抑制BMP诱导的Smad1/5/8活化。DMH1增加小鼠胚胎干细胞中心肌细胞祖细胞,并促进心肌分化。

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).

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.(Only for Reference)

1206711-16-1

C24H20N4O

380.451

DMH1

H2O:<1 mgml
DMSO:21 mg/mL (55.2 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years