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RGFP966 | Inhibitor of HDAC3
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
HDAC3
  • IC50:0.08 uM
  • IC50:1.3 uM
Inhibitor
100 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: Ki - HDAC1: 148 nM

Potency Assay Off-Target:
In Reaction Biology biochemical assay, RGFP966 had no activity on HDACs other than HDAC3 up to 15 uM ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
The related compound (106) was tested in chemoproteomic assays in nuclear extracts. In these experim ...

Potency
Cellular
In Vitro

HDAC3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

In Vivo Validations

C57BL/6J male mice
Dose: 10 mg/mL
Route of delivery: Subcutaneous
Organ of interest (O): brain
Target engagement assay: Not done

Reference: --

Orthogonal Probes def

Romidepsin

Chemical Information

Molecular Formula C21H19FN4O
SMILEs Nc1cc(F)ccc1NC(=O)/C=C/c1cnn(C/C=C/c2ccccc2)c1
InChI InChI=1S/C21H19FN4O/c22-18-9-10-20(19(23)13-18)25-21(27)11-8-17-14-24-26(15-17)12-4-7-16-5-2-1-3-6-16/h1-11,13-15H,12,23H2,(H,25,27)/b7-4+,11-8+
Molecular weight 362.15 Da
AlogP 3.9697000000000022
HBond acceptors 5
HBond donors 3
Atoms 46

References

Publications

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    Vendors

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    Expert Reviews

    by SERP
    (on 26 Apr 2017 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    by SERP
    (on 31 May 2017 )
    Cellular Use Rating
    In Model Organisms
    This is an N-(o-amino-phenyl)carboxamide HDAC3-selective inhibitor with an IC50 of 80 nM and 'no effective inhibition of other HDACs' at concentrations up to 15 uM utilizing a substrate-dependent biochemical...
    by SERP
    (on 12 Jun 2017 )
    Cellular Use Rating
    In Model Organisms
    RGFP966 has been demonstrated to have selective activity for HDAC3 in biochemical assays over most other HDAC enzymes. In cells, Matthews et al., (Blood, 2015) observed that RGFP966 treatment phenocopied...

    Portal Comments

    According to the latest paper from Olsen’s Lab (DOI:10.1021/acsmedchemlett.1c00702) RGFP966 has only a marginal preference for HDAC3 vs HDAC1 and 2, hence it shouldn’t be considered as a selective probe...

    (last updated: 25 May 2022)

    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