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    Dorsomorphin 2HCl (BML275)
    Dorsomorphin 2HCl (BML275)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0246
    CAS #: 1219168-18-9Purity ≥98%

    Description: Dorsomorphin 2HCl (formerly BML-275 dihydrochloride) is a reversible and selective AMPK (AMP-activated protein kinase) inhibitor that inhibits AMPK with a Ki of 109 nM in cell-free assays, exhibiting little inhibition against closely related kinases such as ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin is also an inhibitor of BMP signaling, which promotes cardiomyogenesis in embryonic stem cells. Dorsomorphin reverses the mesenchymal phenotype of breast cancer initiating cells by inhibition of bone morphogenetic protein signaling. 

    References: Nat Chem Biol. 2008 Jan;4(1):33-41; Atherosclerosis. 2011 Nov;219(1):57-64.

    Related CAS #: 866405-64-3 (free base)  

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    Molecular Weight (MW)

    472.41

    Formula

    C24H25N5O.2HCl

    CAS No.

    1219168-18-9

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO:94 mg/mL (199 mM)

    Water: <1 mg/mL

    Ethanol: <1 mg/mL

    Solubility (In vivo)

    PBS: 15 mg/mL

    Synonyms

    Compound C; BML275; BML 275; BML-275; CpdC

    Chemical Name: 6-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-3-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidine dihydrochloride

    InChi Key: RJDVIJJQKMGPMV-UHFFFAOYSA-N

    InChi Code: InChI=1S/C24H25N5O.2ClH/c1-2-12-28(13-3-1)14-15-30-22-6-4-19(5-7-22)21-16-26-24-23(17-27-29(24)18-21)20-8-10-25-11-9-20;;/h4-11,16-18H,1-3,12-15H2;2*1H

    SMILES Code: [H]Cl.[H]Cl.C12=C(C3=CC=NC=C3)C=NN1C=C(C4=CC=C(OCCN5CCCCC5)C=C4)C=N2


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    In Vitro

    In vitro activity: 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.

     

    Kinase Assay: Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6.

     

    Cell Assay: Dorsomorphin (compound C) (0-10 μM, 18 h) suppresses 2DG-induced GRP78 promoter activity in human fibrosarcoma HT1080 cells in a dose-dependent manner but has little effect on tunicamycin-induced GRP78 promoter activity. Dorsomorphin (compound C) C also suppresses GRP78 promoter activity induced by glucose withdrawal. Dorsomorphin (compound C) has no effect on 2DG-induced PERK activation and reduces the both basal and 2DG-induced AMPK phosphorylation levels in HT1080 cells

    In Vivo

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

    Animal model

    Iron-replete mice

    Formulation & Dosage

    Dissolved in DMSO; 10 mg/kg; i.v. administration

    References

    Nat Chem Biol. 2008 Jan;4(1):33-41; Atherosclerosis. 2011 Nov;219(1):57-64. (3):302-15.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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