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    GSK2801 (GSK-2801)
    GSK2801 (GSK-2801)

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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 #: V0419
    CAS #: 1619994-68-1Purity ≥98%

    Description: GSK2801 (GSK-2801) is a novel, orally bioavailable, selective, cell bioactive and acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains, which are the two closely related bromodomain containing proteins BAZ2A and BAZ2B constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC) that regulates the expression of noncoding RNAs. GSK2801 inhibits BAZ2A and BAZ2B with Kd of 257 nM and 136 nM, respectively. It has the potential to be used as a versatile tool compound for cellular and in vivo studies to understand the role of BAZ2 bromodomains in chromatin biology. 

    References: J Med Chem. 2016 Feb 25;59(4):1410-24. 

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    Molecular Weight (MW)371.45
    FormulaC20H21NO4S
    CAS No.1619994-68-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 74 mg/mL (199.2 mM)
    Water: <1 mg/mL
    Ethanol:  7 mg/mL (18.8 mM)
    Solubility (In vivo)0.5% CMC+1% Tween 80: 30mg/mL
    Synonyms

    GSK-2801; GSK 2801; GSK2801

    Chemical Name: 1-(1-(2-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone

    InChi Key: KHWCPNJRJCNVRI-UHFFFAOYSA-N

    InChi Code: InChI=1S/C20H21NO4S/c1-4-11-25-15-9-10-21-18(14(2)22)13-17(19(21)12-15)16-7-5-6-8-20(16)26(3,23)24/h5-10,12-13H,4,11H2,1-3H3

    SMILES Code: CC(C1=CC(C2=CC=CC=C2S(=O)(C)=O)=C3C=C(OCCC)C=CN13)=O 



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    In Vitro

    In vitro activity: In U2OS cells transfected with mutant BAZ2A (N1873F), GSK2801 (1 μM) accelerates FRAP half-recovery time by displacing BAZ2A from chromatin.


    Kinase Assay: GSK2801 is a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd=136 nM) and BAZ2B(Kd=257 nM) bromodomains.


    Cell Assay: In U2OS cells, treatment with the SAHA induced hyperacetylated chromatin. In a GFP-BAZ2A fusion construct, the conserved asparagines that are essential for recognizing the acetylated lysine has been mutated. When a GFP-BAZ2A fusion construct was transfected into SAHA-treated U2OS cells, the mutant construct accelerated FRAP half-recovery time. Treatment with GSK2801 alone in U2OS cells also accelerated FRAP half-recovery time. Both acceleration extents are the same. This meant that GSK2801 can displace BAZ2A from chromatin.

    In VivoIn male CD1 mice, GSK2801 (30 mg/kg, p.o. and i.p.) has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability.
    Animal modelMale CD1 mice
    Formulation & DosageFormulated in 0.5% CMC+1% Tween 80; 30 mg/kg; i.p. or p.o.
    References

    J Med Chem. 2016 Feb 25;59(4):1410-24. 


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

    GSK2801

    Chemoproteomic profiling of BAZ inhibitor selectivity to endogenous bromodomain proteins. J Med Chem. 2016 Feb 25; 59(4): 1410–1424.

    GSK2801

    BAZ2A fluorescence recovery after photobleaching assay. J Med Chem. 2016 Feb 25; 59(4): 1410–1424.


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