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PF-CBP1 | 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
  • IC 50:363 nM
    CREBBP
    • Kd:190 nM
    • IC 50:130 nM
    • Residual activity:49 %
    Antagonist
    100 nM - 1 uM

    Selectivity

    In Vitro Selectivity Assessment

    Potency: IC50

    Potency Assay Off-Target:
    In BROMOscan assay, testing 19 bromodomains, only CBP/EP300 was affected at < 1 uM; BRD4 KD > 20 uM ...
    Selectivity Assessment Description:
    PF-CBP1 displays greater than 100-fold selectivity for the bromodomain of CBP over those of BRD4 and ...

    Potency
    Cellular
    In Vitro

    EP300

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1016/j.chembiol.2015.10.013

    CREBBP

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1016/j.chembiol.2015.10.013

    Negative Control Compounds

    ISOX-INACT (isolipophilic inactive isomer)

    Orthogonal Probes def

    SGC-CBP30
    I-CBP112
    GNE-049

    Chemical Information

    Molecular Formula C29H36N4O3
    SMILEs CCCOc1ccc(CCc2nc3cc(-c4c(C)noc4C)ccc3n2CCN2CCOCC2)cc1
    InChI InChI=1S/C29H36N4O3/c1-4-17-35-25-9-5-23(6-10-25)7-12-28-30-26-20-24(29-21(2)31-36-22(29)3)8-11-27(26)33(28)14-13-32-15-18-34-19-16-32/h5-6,8-11,20H,4,7,12-19H2,1-3H3
    Molecular weight 488.28 Da
    AlogP 5.21434
    HBond acceptors 7
    HBond donors --
    Atoms 72

    Vendors

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

    Expert Reviews

    by SERP
    (on 28 Mar 2017)
    Cellular Use Rating
    The biochemical, cellular and ITC data reported in the reference (Chem Biol 2015, 22, 1588-1596) support the use of PF-CBP1 as a selective probe for the interrogation of the function of CBP bromodomain...
    by SERP
    (on 6 Apr 2017)
    Cellular Use Rating
    I believe this is the best CRBP probe available, but it is far from ideal. It is only weakly potent. Ideally it would be <100 nM but it is only active in cells at or above 1 uM. The margin to BRD4 potency...
    by SERP
    (on 26 Jul 2017)
    Cellular Use Rating
    PF-CBP1 mildly downregulated expression of key inflammatory genes (e.g., IL6, IL1B, IFNB, TNF) in J774, a murine macrophage cell line, at concentrations typically >/=1 uM and did not show cytotoxicity....
    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