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UNC0638 | UNC0638 : Inhibitor of EHMT2 and EHMT1
RATINGS:
Cellular Use: (4 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
EHMT2
  • Kd:27 nM
  • IC 50:<15 nM
  • IC 50:81 nM
EHMT1
  • IC 50:19 nM
    Inhibitor
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    UNC0638 was inactive against other H3K9 (SUV39H1 and SUV39H2), H3K27 (EZH2), H3K4 (SETD7, MLL and SM ...
    Selectivity Assessment Description:
    Selectivity of UNC0638 was evaluated across non-epigenetic targets, including GPCRs, ion channels ...

    Potency
    Cellular
    In Vitro

    EHMT2

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1038/nchembio.599

    EHMT1

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1038/nchembio.599

    In Vivo Validations

    Mouse
    Dose: 1 mg/mL
    Route of delivery: Intravenous
    Plasma half life: 8.8 h
    Systemic clearance: 306 mL/min/kg

    DOI Reference: 10.1038/nchembio.599

    Negative Control Compounds

    QQS

    Orthogonal Probes def

    A-366
    BIX-01294
    UNC0642

    Chemical Information

    Molecular Formula C30H47N5O2
    SMILEs COc1cc2c(NC3CCN(C(C)C)CC3)nc(C3CCCCC3)nc2cc1OCCCN1CCCC1
    InChI InChI=1S/C30H47N5O2/c1-22(2)35-17-12-24(13-18-35)31-30-25-20-27(36-3)28(37-19-9-16-34-14-7-8-15-34)21-26(25)32-29(33-30)23-10-5-4-6-11-23/h20-24H,4-19H2,1-3H3,(H,31,32,33)
    Molecular weight 509.37 Da
    AlogP 5.8355
    HBond acceptors 7
    HBond donors 1
    Atoms 84

    Expert Reviews

    by SERP
    (on 17 May 2016 )
    Cellular Use Rating
    ( The reviewer did not leave any comments )
    by SERP
    (on 25 Apr 2017 )
    Cellular Use Rating
    ( The reviewer did not leave any comments )
    by SERP
    (on 14 Aug 2017 )
    Cellular Use Rating
    In Model Organisms
    I recommend using UNC0638 in parallel with A-366 (as an orthogonal control).
    by SERP
    (on 10 Nov 2020 )
    Cellular Use Rating
    In Model Organisms
    The compound shows inhibitory activity against a few GPCR receptors such as M2, alpha1a and alpha1b at 1 micromolar in vitro, while it is not clear if there is such effect in vivo. So, when you use...
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