Dorsomorphin (Compound C) 2HCl (Synonyms: BML-275 2HCl,Compound C 2HCl) |
رقم الكتالوجGC12560 |
دورسومورفين (كومباوند سي) 2HCl (BML-275 دايهيدروكلورايد؛ كومباوند سي دايهيدروكلورايد) هو مثبط قوي وانتقائي لـ AMPK المتنافس على ATP ، بـ Ki يصل إلى 109 نانومتر. يعمل دورسومورفين (كومباوند سى) 2HCl على تثبيط مسار BMP من خلال استهداف مستقبلات النوع I ALK2 وALK3 وALK6. يحفز دورسومورفین (کامپاییشی C) 2HCl التخرُّج الذاتِــية.
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Cas No.: 1219168-18-9
Sample solution is provided at 25 µL, 10mM.
IC50: Dorsomorphin inhibited BMP4-induced phosphorylation of BMP-responsive SMADs in a dose-dependent manner (half maximal inhibitory concentration (IC50) =0.47 mM).
Bone morphogenetic protein (BMP) signals coordinate developmental patterning and have essential physiological roles in mature organisms. The first known small-molecule inhibitor of BMP signaling, dorsomorphin, were identified in a screen for compounds that perturb dorsoventral axis formation in zebrafish.
In vitro: Previoius researchers found that dorsomorphin selectively inhibits the BMP type I receptors ALK2/ALK3/ALK6 leading to block BMP-mediated SMAD1/5/8 phosphorylation, osteogenic differentiation as well as target gene transcription. Using dorsomorphin, they examined the role of BMP signaling in iron homeostasis.dorsomorphin inhibited the systemic iron regulator hepcidin BMP-, hemojuvelin- and interleukin 6–stimulated expression, indicating that BMP receptors regulate hepcidin induction by all of these stimuli [1].
In vivo: The systemic challenge with iron rapidly induced SMAD1/5/8 phosphorylation and hepcidin expression in the liver, while dorsomorphin treatment could blocke SMAD1/5/8 phosphorylation, normalize hepcidin expression and increase serum iron levels. These suggest an crucial physiological role for hepatic BMP signaling in iron-hepcidin homeostasis [1].
Clinical trial: Dorsomorphin is still in preclinical development stage and no clinicl trial is ongoing currently.
Reference:
[1] Yu PB, Hong CC, Sachidanandan C, Babitt JL, Deng DY, Hoyng SA, Lin HY, Bloch KD, Peterson RT.Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat Chem Biol. 2008;4(1):33-41.
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