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抑制剂描述:

产品名称:Dorsomorphin free base

产品别名:见爱必信

英文别名:Dorsomorphin free base

靶点:AMPK

CAS:866405-64-3

纯度:>98%

外观:见爱必信

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Dorsomorphin(Compound C; BML-275) has been shown to act as a potent and selective inhibitor of AMPK (AMP-activated protein kinase; Ki = 109 nM), induced by AICAR and metformin; also inhibits the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), B

溶解性:DMSO : 3 mg/mL (7.5 mM), warmed
Ethanol : 2 mg/mL (5.0 mM), warmed

体外研究:

Dorsomorphin inhibits ACC inactivation by either AICAR or metformin, and also attenuates AICAR and metformin’s effect to increase fatty acid oxidation or suppress lipogenic genes in hepatocytes. Inhibition of AMPK activity by Dorsomorphin almost completely inhibits autophagic proteolysis in HT-29 cells. in addition, Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6, and thus blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation.

体内研究:Dorsomorphin (10 mg/kg) reduces basal levels of hepcidin expression and increases serum iron concentrations in mice. Dorsomorphin (0.2 mg/kg, i.v.) significantly reduces VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats.

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