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SGC-CBP30 | Antagonist of EP300, CREBBP
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 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
EP300
  • Kd:47 nM
    CREBBP
    • Kd:38 nM
    100 nM - 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    DSF binding assay
    Selectivity Assessment Description:
    In DSF binding assays with 45 bromodomains, SGC-CBP30 had no significant activity except against BRD ...

    Potency
    Cellular
    In Vitro

    EP300

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1073/pnas.1501956112

    CREBBP

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1073/pnas.1501956112

    Negative Control Compounds

    SGC-CBP30N (BDOIA513)
    Notes: SGC-CBP30N (BDOIA513) is the negative control for SGC-CBP30. This compound has moderate activity for CREBBP (Thermal shift 2°C compared to 9.7°C for SGC-CBP30). This compound is inactive against BRD4 (Thermal shift 0.4°C compared to 1.8°C for SGC-CBP30)

    Orthogonal Probes def

    GNE-049
    CPI-1612

    Chemical Information

    Molecular Formula C28H33ClN4O3
    SMILEs COc1ccc(CCc2nc3cc(-c4c(C)noc4C)ccc3n2C[C@H](C)N2CCOCC2)cc1Cl
    InChI InChI=1S/C28H33ClN4O3/c1-18(32-11-13-35-14-12-32)17-33-25-8-7-22(28-19(2)31-36-20(28)3)16-24(25)30-27(33)10-6-21-5-9-26(34-4)23(29)15-21/h5,7-9,15-16,18H,6,10-14,17H2,1-4H3/t18-/m0/s1
    Molecular weight 508.22 Da
    AlogP 5.476040000000006
    HBond acceptors 7
    HBond donors --
    Atoms 69

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the Portal.

    Expert Reviews

    by SERP
    (on 24 May 2016)
    Cellular Use Rating
    Users of this probe are advised to carefully consider the concentration range appropriate for their experiment. Although the recommendation states a 100-1000nM range in cells, pIC50 in a reporter assay...
    by SERP
    (on 14 Jun 2016)
    Cellular Use Rating
    While the existing data suggest this is a high-quality probe, users should realize it was only screened versus 10 representatives within each BRD family, not the entire target class. Also, there is...
    by SERP
    (on 20 Jun 2016)
    Cellular Use Rating
    SGC-CBP30 has BRD4(1) Kd of 850 nM; at 40-fold, this was the largest selectivity window over BET bromodomains reported until recently. BET-family bromodomain inhibitors have strong effects on cell proliferation...
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    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