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    UNC0379
    UNC0379

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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 #: V0392
    CAS #: 1620401-82-2Purity ≥98%

    Description: UNC0379 is a substrate competitive lysine methyltransferase SETD8 (KMT5A) inhibitor with antineoplastic activity. It inhibits KMT5A with an IC50 of 7.9 μM, and shows higher selectivity for  KMT5A over 15 other methyltransferases. 

    References: J Med Chem. 2014 Aug 14;57(15):6822-33.

    Related CAS: 1620401-83-3 (UNC0379 trifluoroacetate salt)

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    Molecular Weight (MW)413.56
    FormulaC23H35N5O2
    CAS No.1620401-82-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: Soluble in DMSO    
    Water: N/A
    Ethanol: N/A
    Solubility (In vivo)Chemical Name: 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine
    InChi Key: WEXCGGWTIDNVNT-UHFFFAOYSA-N
    InChi Code: InChI=1S/C23H35N5O2/c1-29-20-16-18-19(17-21(20)30-2)25-23(28-14-8-9-15-28)26-22(18)24-10-4-3-5-11-27-12-6-7-13-27/h16-17H,3-15H2,1-2H3,(H,24,25,26)
    SMILES Code: COC1=C(OC)C=C(N=C(N2CCCC2)N=C3NCCCCCN4CCCC4)C3=C1  
    SynonymsUNC-0379, UNC 0379, UNC0379


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    In Vitro

    In vitro activity: UNC0379 is competitive with the peptide substrate and noncompetitive with the cofactor SAM


    Kinase Assay: Enzyme assay The interaction between UNC0379 and protein SETD8 was further explored using a ProteOn XPR36 biosensor (Bio-Rad Laboratories, Inc.) at 25 °C. PBS buffer (phosphate buffered saline, pH 7.4) supplemented with 0.005% Tween-20 was used as the running buffer. A GLH (catalog no. 176-5013, Bio-Rad Laboratories, Inc.) sensor chip was first activated by flowing a mixture of 20 mM sulfo-NHS and 20 mM EDC over the chip surface for 5 min at a flow rate of 30 μL/min. SETD8 was then diluted to 20 and 10 μg/mL in 5 mM NaOAc, pH 5.0, and immobilized onto two ligand channels (30 μL/min for 2 min). The surface was then deactivated by flowing 1 M ethanolamine for 5 min at a flow rate 60 μL/min. A blank injection of the running buffer was made, after which four concentrations of the compound in the running buffer (100, 33.3, 11.1, and 3.7 μM) and a running buffer were injected simultaneously at a flow rate of 50 μL/min for 60 s. The sensorgrams obtained at the four concentrations of the compound were fit simultaneously after subtracting a ligand reference (inner spot) and a double compound reference (buffer) using a Langmuir model to obtain on (ka) and off (kd) rates. The kinetic KD was calculated based on the on and off rates for three replicates. An equilibrium analysis of the data was also performed to calculate the KD. 

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    ReferencesJ Med Chem. 2014 Aug 14;57(15):6822-33.


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

    UNC0379

    Compound 1 binds SETD8 with a KD of 18.3 ± 3.2 μM (n = 3) in ITC studies.  2014 Aug 14;57(15):6822-33.

    UNC0379

    Compound 1 was identified as an inhibitor of SETD8 by cross-screening a quinazoline-based inhibitor set.

    UNC0379

    Compound 1 exhibits rapid on and off rates in SPR studies.

    UNC0379

    MOA studies of compound 1.  2014 Aug 14;57(15):6822-33.

    UNC0379

    Peptide displacement assay.  2014 Aug 14;57(15):6822-33.


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