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    PFI-3
    PFI-3

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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 #: V0423
    CAS #: 1819363-80-8Purity ≥98%

    Description: PFI-3 (PFI3) is a potent, selective, acetyl-lysine-competitive, and cell-permeable inhibitor of SMARCA bromodomains (SMARCA2/4 and PB1(5)) with antineoplastic activity. It inhibits SMARCA2/4 bromodomains with Kd values of 55 and 110 nM, respectively.  

    ReferencesCancer Res. 2015 Sep 15;75(18):3865-78;  2016 May 26;59(10):4800-11.

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    Molecular Weight (MW)321.37
    FormulaC19H19N3O2
    CAS No.1819363-80-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 64 mg/mL (199.1 mM)
    Water: <1 mg/mL
    Ethanol:  <1 mg/mL
    SMILES OC1=C(C(/C=C/N2[[email protected]](C3)CN(C4=NC=CC=C4)[[email protected]]3C2)=O)C=CC=C1
    Synonyms PFI 3; PFI3; PFI-3



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    In Vitro

    In vitro activity: PFI-3 shows a significant selectivity for PB1(5) and SMARCA2/4 over 36 other tested kinases.


    Kinase Assay: Using recombinant purified bromodomains, we discovered that PFI-3 binds with similar avidity to both the short and long isoform of SMARCA2 revealing that the alternatively-spliced 18 amino acid insert does not impair PFI-3 binding. Moreover, profiling against 32 bromodomains at DiscoveRx confirmed exquisite selectivity vs. other subfamilies expanding the PFI-3 selectivity information obtained using differential scanning fluorimetry (DSF). In summary, we find there is a good concordance between the ligand competition (BROMOScan) and the direct biophysical binding (DSF) assays and note that in addition to targeting SMARCA2/4, PFI-3 also has activity (~70% inhibition at 2 uM) against the structurally related fifth bromodomain from PBRM1, another SWI/SNF subunit.


    Cell Assay: In cell-based chromatin binding assays, using in situ cell extraction techniques to remove non-chromatin bound proteins, we observed dose-dependent displacement of GFP-tagged SMARCA2 bromodomain (i.e. 132 amino acid residues) by PFI-3. Notably, the inhibitor showed prolonged cell-target engagement with similar potency (IC50 = 5.78 uM) following 2 and 24 hours treatment. As a negative control, JQ1 did not inhibit the binding of ectopically expressed SMARCA2 bromodomain, but selectively displaced GFP-tagged BRD4 (data not shown). Taken together, our cell-biochemical data cooperate the accelerated fluorescence recovery after photobleaching (FRAP) reported for PFI-3 and we conclude that PFI-3 is a selective, cell-permeable probe suitable to study the inhibition of SMARCA2/4 bromodomains in cells.

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    References

     Cancer Res. 2015 Sep 15; 75(18): 3865–3878.


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

    PFI-3

    Pharmacological inhibition of SMARCA2/4 bromodomain in lung cancer. Cancer Res. 2015 Sep 15; 75(18): 3865–3878.

    PFI-3

    Pharmacological inhibition of SMARCA2/4 bromodomain in lung cancer. Cancer Res. 2015 Sep 15; 75(18): 3865–3878.

    PFI-3

    PFI-3 is a potent, selective and cell permeable bromodomain inhibitor of SMARCA2/4. Cancer Res. 2015 Sep 15; 75(18): 3865–3878.


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