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  • 产品名称: Dorsomorphin
  • 产品货号: CS1977
  • 货期: 现货
  • 价格与订购: 580
  • 数量:
    库存: 100
  • 规格: 5mg 10mg 1g
  • 产品信息
  • 如何订购
    产品描述
    Dorsomorphin is an effective and specific inhibitor of AMPK (AMP-activated protein kinase), which is induced by AICAR and metformin.
    靶点活性
    AMPK
    体外活性
    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. [1] Inhibition of AMPK activity by Dorsomorphin almost completely inhibits autophagic proteolysis in HT-29 cells. [2] 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. [3] 
    体内活性
    Dorsomorphin (10 mg/kg) reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice. [3] Dorsomorphin (0.2 mg/kg, i.v.) significantly reduces VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats. [4] 
    激酶实验
    HT1080 cells are seeded in 24-well plates (2×104 cells per well) and treated with Dorsomorphin in the presence or absence of glucose or 10 mM 2DG for 2 h. HT1080 cells that overexpressed the wild-type and dominant negative AMPKα1 are prepared by transfecting plasmid DNA (pAMPKα1-wt, pAMPKα1-D168A and pcFlag as a control) in 6-well plates, seeding in 24-well plate and treating with UPR inhibitors. Cells are lysed with cell lysis buffer (20 mM Tris-HCl, pH 7.5, 250 mM NaCl, 10% glycerol, 0.5% NP-40, 1 mM EDTA, 1 mM EGTA, 0.2 mM PMSF, 1 µg/mL pepstatin, 0.5 µg/mL leupeptin, 5 mM NaF, 2 mM Na3Vo4, 2 mM β-glycerophosphate, 1 mM DTT). Relative AMPK kinase activity (mean±SD of duplicate determinations) to control sample (vehicle or pcFlag under normal growth conditions) is determined using the CycLex AMPK kinase assay kit[2].
    细胞实验
     Dorsomorphin is dissolved in DMSO (10 mM) and stored,and then diluted with appropriate media (DMSO 0.5%) before use[2].HeLa and 786-O cells are treated with various concentrations of Dorsomorphin (0,0.3,1,3,10 μM ),Versipelostatin and Phenformin in the presence or absence of 10 mM 2DG or 1 µg/mL of Tunicamycin as a stressor for 30 h in 96-well plates.For the combination study,786-O cells are treated with various concentrations of UPR inhibitors in the presence or absence of 10 mM 2DG for 24 h.The medium is then replaced with fresh growth medium,and cells are cultured for a further 15 h.Subsequently,MTT is added to the culture medium,and the absorbance of each well is determined.For the viability assay under glucose-withdrawal conditions,HT1080 cells are treated with various concentrations of Dorsomorphin and phenformin in 12-well plates in the presence or absence of glucose for 18 h,seeded in 96-well plates with growth medium,and then cultured for a further 48 h before MTT is added.Relative cell survival (mean±SD of quadruplicate determinations) is calculated by setting each control absorbance from untreated cells as 100%.The effects of drug combinations at concentrations producing 80% cell growth inhibition (IC80) are analyzed using the isobologram method[2]. Cell lines:icon
    参考文献
    1. Zhou G, et al. J Clin Invest. 2001, 108(8), 1167-1174.
    2. Meley D, et al. J Biol Chem. 2006, 281(46), 34870-34879.
    3. Yu PB, et al. Nat Chem Biol. 2008,
    4(1), 33-41.4. Kim YM, et al. Atherosclerosis. 2011, 219(1), 57-64.
    5. Ma L, Gong F, Xu J, et al. Uncarboxylated osteocalcin reverses the high glucose‑induced inhibition of the osteogenic differentiation of MC3T3E1 cells via the GPRC6A/cAMP/PKA/AMPK signaling pathway[J]. International Journal of Molecular Medicine. 2021, 47(5): 1-11
    6. He Y, Xu K, Wang Y, et al. AMPK as a potential pharmacological target for alleviating LPS-induced acute lung injury partly via NLRC4 inflammasome pathway inhibition[J]. Experimental Gerontology. 2019: 110661.
    7. Yang, Feihong, et al. Vaspin alleviates myocardial ischaemia/reperfusion injury via activating autophagic flux and restoring lysosomal function [J]. Biochemical and biophysical research communications. 2018 Sep 5;503(2):501-507.
    8. Wang X D, Yu W L, Sun Y. Activation of AMPK restored impaired autophagy and inhibited inflammation reaction by up-regulating SIRT1 in acute pancreatitis[J]. Life Sciences. 2021: 119435.
    9. Wu Y, Zeng S, Wan B, et al. Sophoricoside attenuates lipopolysaccharide-induced acute lung injury by activating the AMPK/Nrf2 signaling axis[J]. International Immunopharmacology. 2021, 90: 107187
    10. Wu Y, Zeng S, Wan B, et al. Sophoricoside attenuates lipopolysaccharide-induced acute lung injury by activating the AMPK/Nrf2 signaling axis[J]. International Immunopharmacology. 2020: 107187.
    别名
    Compound C , BML-275
    纯度
    99.48% 
    分子量
    399.49
    分子式
    C24H25N5O 
    CAS No
    866405-64-3 
    存储
    Powder: -20°C for 3 years
    In solvent: -80°C for 6 months
    溶解度
    DMSO: 10mM
    ( < 1 mg/ml refers to the product slightly soluble or insoluble )
    icon
    Note
    For research use only .