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VZ185 | Degrader (PROTAC) of BRD7, BRD9
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
BRD7
    • DC 50:4.5 nM
    • Dmax:95%
    BRD9
    • Kd:26 ± 9 nM binary, 27 ± 3nM Ternary
    • DC 50:1.8 nM
    • Dmax:95%
    Degrader (PROTAC)
    up to 300 nM

    Selectivity

    In Cell Selectivity Assessment
    Selectivity Assessment Description:
    Selectivity tested via multiplexed isobaric tagging MS proteomic experiments.

    Potency
    Cellular
    In Vitro

    BRD7

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.8b01413

    BRD9

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.8b01413

    Negative Control Compounds

    cis-VZ185

    Orthogonal Probes def

    LP99

    Chemical Information

    Molecular Formula C53H67FN8O8S
    SMILEs COc1cc(-c2cn(C)c(=O)c3cnccc23)cc(OC)c1CN1CCN(CCCCCOc2cc(-c3scnc3C)ccc2CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)CC1
    InChI InChI=1S/C53H67FN8O8S/c1-33-46(71-32-57-33)34-11-12-35(27-56-48(64)42-26-37(63)29-62(42)50(66)47(52(2,3)4)58-51(67)53(54)14-15-53)43(23-34)70-22-10-8-9-17-60-18-20-61(21-19-60)31-41-44(68-6)24-36(25-45(41)69-7)40-30-59(5)49(65)39-28-55-16-13-38(39)40/h11-13,16,23-25,28,30,32,37,42,47,63H,8-10,14-15,17-22,26-27,29,31H2,1-7H3,(H,56,64)(H,58,67)/t37-,42+,47-/m1/s1
    Molecular weight 994.48 Da
    AlogP 0.0
    HBond acceptors 16
    HBond donors 3
    Atoms 138

    Vendors

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    Expert Reviews

    by SERP
    (on 26 Feb 2021 )
    Cellular Use Rating
    VZ185 is a new high-quality chemical degrader probe of BRD9 and BRD7. Its target binding and cellular effects have very convincingly been demonstrated. In vivo data have not been shown in the original...
    by SERP
    (on 12 Mar 2021 )
    Cellular Use Rating
    VZ185 together with its published inactive control is an excellent degrader of the bromodomain proteins BRD7 and BRD9. MS based experiments showed that this PROTAC is highly selective and potent. Experimental...
    by SERP
    (on 12 Mar 2021 )
    Cellular Use Rating
    VZ185 is a potent and effective degrader of BRD7 and BRD9 in cells. The activity of VZ185 has been clearly linked to the binding to BRD7 and 9 as well as VHL. Convincing time-course and dose-response...
    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