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A-485 | Inhibitor of EP300, CREBBP
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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 50:9.8 nM
  • Kd:15 nM
  • EC50:73 nM
CREBBP
  • IC 50:2.6 nM
    Inhibitor
    800 nM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    A-485 was assayed against other HAT family members and did not inhibit the activity of p300/CBP-a ...
    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    Selective against BRDs (BRD3, BRD4, BRDT), Kinases (78) and common targets (CEREP) except for the ...

    Potency
    Cellular
    In Vitro

    EP300

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.biochem.7b01179

    CREBBP

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.biochem.7b01179

    In Vivo Validations

    Mouse
    Dose: 50, 100, 200, 500 mg/kg
    Route of delivery: Intraperitoneal, Oral
    Plasma half life: from 1.3 to 3 h

    DOI Reference: 10.1038/nature24028

    Negative Control Compounds

    A-486

    Orthogonal Probes def

    GNE-049
    CPI-1612
    SGC-CBP30

    Chemical Information

    Molecular Formula C25H24F4N4O5
    SMILEs CNC(=O)Nc1ccc2c(c1)CC[C@@]21OC(=O)N(CC(=O)N(Cc2ccc(F)cc2)[C@@H](C)C(F)(F)F)C1=O
    InChI InChI=1S/C25H24F4N4O5/c1-14(25(27,28)29)32(12-15-3-5-17(26)6-4-15)20(34)13-33-21(35)24(38-23(33)37)10-9-16-11-18(7-8-19(16)24)31-22(36)30-2/h3-8,11,14H,9-10,12-13H2,1-2H3,(H2,30,31,36)/t14-,24+/m0/s1
    Molecular weight 536.17 Da
    AlogP 3.6769
    HBond acceptors 9
    HBond donors 2
    Atoms 62

    Vendors

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

    Expert Reviews

    by SERP
    (on 4 Jun 2020 )
    Cellular Use Rating
    In Model Organisms
    This molecule showed good effect to block H3K27Ac in cells. The compound works well in cell and showed great potency in multiple cell lines. This probe is a great chemical tool to study biological function...
    by SERP
    (on 15 Jun 2020 )
    Cellular Use Rating
    In Model Organisms
    Attention should be paid to the difference between the cellular activity (H3K27Ac) EC50 of 73 nM and the recommended cell assay use concentration of 800 nM. This difference of approximately 10-fold...
    by SERP
    (on 7 Jul 2020 )
    Cellular Use Rating
    In Model Organisms
    A-485 is a well optimized inhibitor of the acetyltransferase EP300/CREBBP. Its on-target activity is well verified in several peer-reviewed manuscripts. Its cell-based activity versus its target occurs...
    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