Romidepsin

Noncovalent inhibitor of HDAC1, HDAC2, HDAC3, HDAC8

Structure

Information

Protein target names: HDAC1, HDAC2, HDAC3, HDAC8

Mechanism of action: Noncovalent inhibitor

Recommended in-cell concentration:
1-100 nM
Primary References:

In Vitro Validations

Uniprot ID: Q13547
Target Class: Epigenetic
Target SubClass: HDAC
Potency: IC50
Potency Value: 36 nM
Potency Assay: HDAC-inhibitory activity was evaluated by using HDACs prepared from 293T cells
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Histone deacetylase 1, RPD3L1, HDAC1, HDAC1_HUMAN, ...

PMID Reference: 12208741

Uniprot ID: Q13547
Target Class: Epigenetic
Target SubClass: HDAC
Potency: Ki
Potency Value: 0.015
Potency Assay: In biochemical enzyme assays with synthetic substrates, FK-228 potently and selectively inhibited class I HDACs
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Histone deacetylase 1, RPD3L1, HDAC1, HDAC1_HUMAN, ...

DOI Reference: 10.1038/nchembio.313

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 26 Apr 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Romidepsin is undoubtedly a useful probe, especially for understanding and comparing relative selectivity across different HDAC family members (cf. PMID 20139990) , because it displays a range of activities against these family members, spanning almost 6 orders of magnitude. A few caveats should be kept in mind when using this compound in cells or animals: 1) because of its activity against many HDACs, it is probably best used as part of a panel of agents in comparison with other more selective compounds; 2) while the concentrations recommended are correct for mammalian cells, earlier work in yeast suggests that with yeast cells a higher concentration might be needed (>10 uM); and 3) as an approved drug, romidepsin is associated with a number of adverse effects, which makes its use as an in vivo research probe questionable.

(last updated: 27 Jun 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Romidepsin is a highly potent probe of class I histone deacetylases with cellular activity in the low nanomolar range. It is suitable for in vivo experiments.

(last updated: 18 Jul 2017 )