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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