ドルソモルヒン 化学特性,用途語,生産方法
外観
白色～黄色, 結晶～粉末
使用上の注意
不活性ガス封入
使用
A potent inhibitor of AMPK and fatty acid biosynthesis.
定義
ChEBI: A pyrazolopyrimidine that is pyrazolo[1,5-a]pyrimidine which is substituted at positions 3 and 6 by pyridin-4-yl and p-[2-(piperidin-1-yl)ethoxy]phenyl groups, respectively. It is a potent, selective, reversible, and ATP-competiti
e inhibitor of AMPK (AMP-activated protein kinase, EC 2.7.11.31) and a selective inhibitor of bone morphogenetic protein (BMP) signaling.
一般的な説明
A cell-permeable pyrrazolopyrimidine compound that inhibits against KDR/VEGFR2, ALK2/BMPR-I, AMPK kinase activity (IC
50 = 25.1, 148, and 234.6 nM, respectively), while exhibiting much reduced or little effect toward ALK5/TGFβR-I, ZAPK, Syk, PKCθ, PKA, or JAK3. Shown to block both BMP pathway-dependent dorsoventral development (EC
100 = 2.5 μM) and VEGF signaling-dependent intersomitic vessel formation (EC
50 = 5 μM) in zebrafish embryo
in vivo. Commonly used in combination with AMPK activators AICAR (Cat. No.
123040) and/or Metformin (Cat. No.
317240) for studying AMPK-dependent cellular events
in vitro and physiological responses in animals
in vivo.
生物活性
Potent and selective inhibitor of AMP-activated protein kinase (AMPK) (K i = 109 nM). Displays no significant activity on several structurally related kinases including ZAPK, SYK, PKC θ , PKA and JAK3. Inhibits AMPK activation induced by AICAR and metformin. Also inhibits bone morphogenic protein (BMP) type I receptors (ALK2, ALK3 and ALK6). Promotes cardiomyogenesis in mouse embryonic stem cells (ESCs) in vitro .
ドルソモルヒン 上流と下流の製品情報
原材料
準備製品