DMH1性质、用途与生产工艺
DMH1是选择性BMP receptor抑制剂,抑制ALK2,IC50为107.9 nM,对AMPK, ALK5, KDR (VEGFR-2)和PDGFR没有抑制效果。
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.
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.
DMH1是选择性BMP receptor抑制剂,抑制ALK2,IC50为107.9 nM,对AMPK, ALK5, KDR (VEGFR-2)和PDGFR没有抑制效果。DMH1可抑制自噬。
Target | Value |
ALK2
(Cell-free assay)
|
107.9 nM
|
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。此外,DMH1作为一种BMP抑制剂,显著降低NSCLC细胞生长,迁移和侵袭。
DMH1使斑马鱼胚胎的胚胎轴背部化,而不破坏血管生成过程。在前心外膜移植组织中,DMH1引起对上皮细胞层迁移的最大抑制。在负荷A549异种移植物的小鼠体内,DMH1 (5 mg/kg i.p.)减弱异种移植肺肿瘤的生长。
DMH1
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