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    GSK621
    GSK621

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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 #: V0249
    CAS #: 1346607-05-3Purity ≥98%

    Description: GSK621 is a novel, potent and selective activator of AMP-activated protein kinase (AMPK) with potential antitumor activity. It selectively kills acute myeloid leukemia (AML) cells but spares normal hematopoietic progenitors. It showed potent antiproliferative activity in vitro and high antitumor efficacy in vivo.

    References:Cell Rep. 2015 Jun 9;11(9):1446-57.

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    Molecular Weight (MW)

    489.91

    Formula

    C26H20ClN3O5

    CAS No.

    1346607-05-3

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 97 mg/mL (198.0 mM)

    Water:<1 mg/mL

    Ethanol:<1 mg/mL

    Solubility (In vivo)

    2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL

    Other info

    Synonym: GSK-621; GSK621; GSK 621.

    Chemical Name: 6-chloro-5-(2'-hydroxy-3'-methoxy-[1,1'-biphenyl]-4-yl)-3-(3-methoxyphenyl)-1,5-dihydro-2H-pyrrolo[3,2-d]pyrimidine-2,4(3H)-dione

    InChi Key: KURYSXLJGKKDHT-UHFFFAOYSA-N

    InChi Code: InChI=1S/C26H20ClN3O5/c1-34-18-6-3-5-17(13-18)30-25(32)23-20(28-26(30)33)14-22(27)29(23)16-11-9-15(10-12-16)19-7-4-8-21(35-2)24(19)31/h3-14,31H,1-2H3,(H,28,33)

    SMILES Code: O=C1NC2=C(N(C3=CC=C(C4=CC=CC(OC)=C4O)C=C3)C(Cl)=C2)C(N1C5=CC=CC(OC)=C5)=O


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    In Vitro

    In vitro activity: In AML cell lines and primary AML samples, GSK621 markedly increases phosphorylation at AMPKα T172, a marker of AMPK activation. In a set of 20 cell lines, GSK621 reduces the proliferation of all 20 lines with IC50 ranged from 13-30 μM, and increases apoptosis in 17 (85%) lines. In addition, GSK621 also triggers autophagy, which partially contributes to AML cell death.

     

    Kinase Assay: HEPG2 cells are treated with increasing doses of A-769662 or GSK621, and ACC S79 phosphorylation is assessed as a surrogate marker for AMPK activation using a commercially available ELISA kit.

     

    Cell Assay: Twenty AML cell lines  (MV4-11, OCI-AML3, OCI-AML2, HL-60, Kasumi, HEL, UT7, NB4, TF-1, KG1A, Nomo p28, SKM-1, U937, YHP1, MOLM-14, Mo7e, K562, MOLM-13, EOL-1, SET-2 cell lines) are treated with log10 dilutions of GSK621 and relative viability is determined by CellTiter-Glo?assay. IC50 of GSK621 among these 20 cell lines is calculated using the Prism software and are presented as log[C] with [C] in mol/l (M). Results are presented for 5 different cell lines per panel.

    In Vivo

    In nude mice bearing MOLM-14 xenografts, GSK621 (30 mg/kg, i.p.) reduces leukemia growth and significantly extends survival by enhancing AMPK activity and the induction of apoptosis.

    Animal model

    In animals with xenograft MOLM-14 cells

    Formulation & Dosage

    30 mg/kg; i.p. injection.

    References

    Cell Rep. 2015 Jun 9;11(9):1446-57.


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

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