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TP-472 | TP-472 : Inhibitor of BRD9, BRD7
RATINGS:
Cellular Use: (2 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
BRD9
  • ΔTm:9.9 °C
  • Kd:82 nM
  • EC50:320 nM
BRD7
  • ΔTm:9.6 °C
  • Kd:556 nM
    Inhibitor
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    No binding to any BRD in a panel of >40 BRD in thermal shift assay with exception of BRD7 and BRD9. ...

    Potency
    Cellular
    In Vitro

    BRD9

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.9b01980

    BRD7

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.9b01980

    Negative Control Compounds

    TP-472N
    Notes: TP472N is inactive against other bromodomains (>20uM against BRD9)

    Orthogonal Probes def

    BI-9564
    VZ185

    Chemical Information

    Molecular Formula C20H19N3O2
    SMILEs CC(=O)c1cc(-c2cc(C(=O)NC3CC3)ccc2C)c2ncccn12
    InChI InChI=1S/C20H19N3O2/c1-12-4-5-14(20(25)22-15-6-7-15)10-16(12)17-11-18(13(2)24)23-9-3-8-21-19(17)23/h3-5,8-11,15H,6-7H2,1-2H3,(H,22,25)
    Molecular weight 333.15 Da
    AlogP 3.4045200000000024
    HBond acceptors 5
    HBond donors 1
    Atoms 44

    Vendors

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

    Expert Reviews

    by SERP
    (on 22 Nov 2022 )
    Cellular Use Rating
    This probe shows reasonable on-target potency against BRD9 (33nM by ITC, 368nM in HEK293 cells by NanoBRET) and a very clean selectivity profile, with BRD7 (340nM by ITC) the only significant off-target...
    by SERP+
    (on 22 Mar 2023 )
    Cellular Use Rating
    The probe characterisation would benefit from cytotoxicity assessment. No publications are available so far (for in-cell data and target engagement) but these can be found on the SGC website.

    Portal Comments

    In a 2023 study, Hu et al. evaluated TP-472 in live-cell assays for Phospholipidosis induction, cautioning about adverse effects at concentrations near 1 uM. (DOI:10.1016/j.chembiol.2023.09.003)

    (last updated: 7 Nov 2023)

    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