Dorsomorphin dihydrochloride is a potent inhibitor of AMP-activated protein kinase (AMPK) (Ki = 109 nM) and bone morphogenic protein (BMP) signaling. Dorsomorphin dihydrochloride inhibits AMPK activation induced by AICAR and metformin. Dorsomorphin dihydrochloride also inhibits the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), BMPR-IA (ALK3), and BMPR-IB (ALK6). Dorsomorphin dihydrochloride induces autophagy in cancer cell lines via a mechanism independent of AMPK inhibition.
|Cell lines||Spermatogonial Cell|
|Preparation method||Dorsomorphin was added to the medium at a final concentration of 0, 1, 2, 4, or 8 µM (in final 0.4% dimethyl sulfoxide). The cells were maintained at 28.5°C in an atmosphere of 3% carbon dioxide and the medium was replaced every 3–4 days.|
|Concentrations||0, 1, 2, 4, or 8 µM|
|Incubation time||3 weeks|
|Animal models||C57BL/6 mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||Water 94 mg/mL|
|Source||Hum Mol Genet (2016). Figure 2. Dorsomorphin dihydrochloride|
|Cell Lines||iPSC lines|
|Incubation Time||72 h|
|Results||We generated cortical neurons using a well-established protocol with small molecule dual SMAD inhibition for neural induction followed by plating of neuroepithelial cells for final differentiation|
Dorsomorphin promotes survival and germline competence of zebrafish spermatogonial stem cells in culture.
Wong TT, et al. PLoS One. 2013 Aug 1;8(8):e71332. PMID: 23936500.
Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism.
Yu PB, et al. Nat Chem Biol. 2008 Jan;4(1):33-41. PMID: 18026094.
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