Dorsomorphin (Compound C) 2HCl (Synonyms: BML-275 2HCl,Compound C 2HCl) |
Catalog No.GC12560 |
도르소모르핀 (컴파운드 C) 2HCl (BML-275 디하이드로클로라이드; 컴파운드 C 디하이드로클로라이드)는 강력하고 선택적인 ATP 경쟁 AMPK 억제제입니다. Ki 값은 109 nM입니다. 도르소모르핀 (컴파운드 C) 2HCl은 유형 I 수용체 ALK2, ALK3 및 ALK6을 대상으로 BMP 신호전달 경로를 억제합니다. 도르소모르핀 (컴파운드 C) 2HCl은 자가포식을 유발시킵니다.
Products are for research use only. Not for human use. We do not sell to patients.
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.
Average Rating: 5
(Based on Reviews and 10 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *