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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

Targets Biochemical/Biophysical Potency Cellular Potency
EP300
  • Kd:47 nM
    CREBBP
    • Kd:38 nM
    Antagonist
    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)
    InChI: InChI=1S/C28H32ClN3O3/c1-19-28(20(2)35-30-19)22-6-8-26-23(17-22)18-24(32(26)11-10-31-12-14-34-15-13-31)7-4-21-5-9-27(33-3)25(29)16-21/h5-6,8-9,16-18H,4,7,10-15H2,1-3H3

    Orthogonal Probes def

    GNE-049
    CPI-1612
    I-CBP112

    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 5.47604
    HBond acceptors 7
    HBond donors --
    Atoms 69

    Vendors

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    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...
    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