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    PFI-2
    PFI-2

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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 #: V0397
    CAS #: 1627676-59-8Purity ≥98%

    Description: PFI-2 (PFI2) is a novel, potent and selective inhibitor of lysine methyltransferase SETD7 [SET domain containing (lysine methyltransferase) 7] with anticancer activity. It inhibits SETD7 with a Ki (app) and IC50 of 0.33 nM and 2 nM, respectively, and shows >1000-fold selectivity for SETD7 over other methyltransferases and other non-epigenetic targets. In HEK293 cells, (R)-PFI-2 (10 µM) bound to and stabilized SETD7. In Setd7+/+ murine embryonic fibroblasts (MEFs), (R)-PFI-2 increased nuclear localization of Yes-associated protein (YAP) and the expression of YAP target genes Ctgf, Gli2 and Cdc20.

    References: Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8.

    Related CAS #: 1627676-59-8 (free base); 1627607-87-7 (HCl)

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    • 香港大学
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    Molecular Weight (MW)499.52
    FormulaC23H25F4N3O3S
    CAS No.1627676-59-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 99 mg/mL (198.2 mM)
    Water: 4 mg/mL (8.0 mM)
    Ethanol: 66 mg/mL (132.1 mM) 
    Other info

    Chemical Name: (R)-8-fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide hydrochloride

    InChi Key: ZADKZNVAJGEFLC-ZMBIFBSDSA-N

    InChi Code: InChI=1S/C23H25F4N3O3S.ClH/c24-20-13-18(12-16-6-7-28-14-19(16)20)34(32,33)29-21(22(31)30-8-1-2-9-30)11-15-4-3-5-17(10-15)23(25,26)27;/h3-5,10,12-13,21,28-29H,1-2,6-9,11,14H2;1H/t21-;/m1./s1

    SMILES Code: O=S(C1=CC2=C(CNCC2)C(F)=C1)(N[[email protected]](CC3=CC=CC(C(F)(F)F)=C3)C(N4CCCC4)=O)=O.[H]Cl

    SynonymsPFI-2 hydrochloride; PFI 2; PFI2; PFI-2; (R)-PFI-2; (R)-PFI-2 hydrochloride. 


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    In Vitro

    In vitro activity: (R)-PFI-2 shows 500-fold more inhibitory activity against human SETD7 than its enantiomer, (S)-PFI-2. In a cellular environment, through direct interactions with SETD7, affects Yes-Associated protein localization and phenocopies Setd7 genetic deletion on Hippo pathway signaling.


    Kinase Assay:  The reaction mixtures containing 2 nM SETD7, 2 uM biotinylated peptide H3 (1-25) and 2 uM SAM in 20 mM Tris, pH 8, 5 mM DTT and 0.01% Triton X-100 were incubated for 1 hour at 23°C. Compound concentration was varied from 0.3 nM to 5 uM. All reactions (in 10 ul) started by adding 3H-SAM and stopped by addition of 10 ul of 7.5 M guanidine hydrochloride. 60 ul of buffer (20 mM Tris, pH 8) was added, mixed and transferred to a 384-well FlashPlate (Cat. # SMP410A001PK; Perkin Elmer; www.perkinelmer.com). The reaction mixtures in Flash plate were incubated for 1 hour and the CPM counts were measured using Topcount plate reader ((Perkin Elmer, www.perkinelmer.com). The CPM counts in the absence of compound for each data set were defined as 100% activity. In the absence of the enzyme, the CPM counts in each data set were defined as background (0%). The IC50 values were determined using GraphPad Prism 6 with Sigmoidal 4PL equation. Cell assay [1] Compound stability was checked in the media with and without cell. Samples were analyzed using Waters Synapt G2 S Quadruple Time-of-flight (Q-Tof) hybrid mass spectrometer (MS) system coupled with second generation ACQUITY ultra-performance liquid chromatography (UPLC-II). Chromatographic separations were carried out on an ACQUITY UPLC BEH C18 (2.1 X 50 mm, 1.7 um) column. The mobile phase was 0.1% formic acid in water (solvent A) and 0.1% formic acid in acetonitrile (solvent B). Compound concentrations were measured as relative peak areas at various time points. 

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    References

    Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8.


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

     

    PFI-2

    Inhibition of Setd7 affects YAP in MEFs and MCF7 cells. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8.



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