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    SGC707
    SGC707

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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 #: V0383
    CAS #: 1687736-54-4Purity ≥98%

    Description: SGC707 (SGC-707) is a novel, cell-permeable and allosteric PRMT3 inhibitor (protein arginine methyltransferase 3 inhibitor) with potential anticancer activity. It inhibits PRMT3 with an IC50 and a Kd of 31 nM and 53 nM, respectively. PRMT3 is involved in cancer development via interaction with the DAL-1 tumor suppressor protein. SGC707 is a chemical probe acting by inhibiting the activity of PRMT3 via targeting the dimerization interface of PRMT3.

    References: Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70; Epigenomics. 2015;7(8):1327-38.

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    Molecular Weight (MW)298.34
    FormulaC16H18N4O2
    CAS No.1687736-54-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 59 mg/mL (197.7 mM)
    Water: <1 mg/mL
    Ethanol: 59 mg/mL (197.7 mM)
    Other info

    Chemical Name: N-6-isoquinolinyl-N'-[2-oxo-2-(1-pyrrolidinyl)ethyl]-urea

    InChi Key: DMIDPTCQPIJYFE-UHFFFAOYSA-N

    InChi Code: InChI=1S/C16H18N4O2/c21-15(20-7-1-2-8-20)11-18-16(22)19-14-4-3-13-10-17-6-5-12(13)9-14/h3-6,9-10H,1-2,7-8,11H2,(H2,18,19,22)

    SMILES Code: O=C(NCC(N1CCCC1)=O)NC2=CC3=C(C=NC=C3)C=C2

    Synonyms

    SGC707; SGC 707; SGC-707


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    In Vitro

    In vitro activity: In cells, SGC707 binds to PRMT3 and reduces PRMT3-dependent H4R3me2a. SGC707 also stabilizes PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM, respectively.


    Kinase Assay: A radioactivity-based assay is optimized and used to determine the inhibition of PRMT3 in vitro. In a scintillation proximity assay (SPA), tritiated S-adenosylmethionine (3H-SAM) served as a methyl donor to methylate biotinylated histone peptide substrate. After completion of the reaction, the reaction mixture is transferred to the wells of a streptavidin / scintillant-coated microplate. The Biotinylated peptides binding to streptavidin coated resin, brings the incorporated 3H-methyl and the scintillant to close proximity. The amount of methylated peptide is quantified by tracing the radioactivity (counts per minute) as measured by the TopCount NXT™ Microplate Scintillation and Luminescence Counter. Due to the very acidic nature of the 3H-SAM solution, non-tritiated (cold) SAM is used to supplement the reactions. The C-terminally biotinylated peptide composed of the first 24 amino acids residues of histone H4 (H4 1-24) is used as substrate. The typical assay mixture contained 0.01% Tween-20, 5 mM DTT, 20 nM PRMT3, 0.3 µM B-H4 1-24 and 28 µM (5 µM3H-SAM plus 23 µM cold SAM) SAM in 20 mM Tris-HCl (pH 7.5) and a final volume of 20 µL. The IC50 values are determined at Km concentrations of both substrates by titration of the compound in the reaction mixture in a range between 2000-0.2 nM.


    Cell Assay: Cells (LnCap, U2O s, HFF, MCF-7, and MDA-MB-231 cells) are seeded in 96-well plates and treated with different concentrations of SGC707 for 72 h. Cell viability is determined using Alamar blue 0.01 mg/mL in the media. Resazurin reduction is monitored with 544 nm excitation, measuring fluorescence at 590 nm.

    In VivoIn CD-1 male mice, SGC707 (30 mg/kg, i.p.) gives good plasma exposure over 6 h with the peak plasma level of 38000 nM, which suggests that SGC707 is suitable for animal studies
    Animal modelMice
    Formulation & Dosage30 mg/kg, i.p.
    References

    Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70; Epigenomics. 2015;7(8):1327-38.


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

     

    SGC707

    SGC707 binds to PRMT3 in cells and reduces PRMT3-dependent H4R3me2a. Angew Chem Int Ed Engl. 2015 Apr 20; 54(17): 5166–5170.



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