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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

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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

    UNC0737

    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 public comments)
    by SERP
    (on 25 Apr 2017)
    Cellular Use Rating
    (The reviewer did not leave any public 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...
    Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria