Romidepsin

Reagent Authentication Certificate:

Chemical Probes Portal Romidepsin.pdf

Protein target name:

HDAC1, HDAC2, HDAC3, HDAC8

Mechanism of action:

Noncovalent inhibitor

Recommended Concentration for use in cells:

1-100 nM

Probe Availability

MedChem Express (128517-07-7)

Tocris (128517-07-7)

Abcam (128517-07-7)

Probe Information

Target and Probe Information

Target Details

Target class:

Epigenetics

Subclass:

HDAC

HUGO ID:

HGNC:4852 HGNC:4853 HGNC:4854 HGNC:13315

Entrez gene ID:

3065 3066 8841 55869

UNIPROT ID:

Q13547 Q92769 O15379 Q9BY41

Target alias:

Histone deacetylase 1, GON-10, HD1, RPD3, RPD3L1, histone deacetylase 2, HD2, RPD3, YAF1, histone deacetylase 3, HD3, RPD3, RPD3-2, histone deacetylase 8, CDA07, CDLS5, HD8, HDACL1, MRXS6, RPD3, WTS, class I HDAC

Probe Details

Chemical Probes Portal ID:

CPP1509

Probe alias:

Depsipeptide; Chromadax; FK228; Antibiotic FR 901228; Istodax, FK 228

PubChem CID:

5352062

ChEMBL ID:

CHEMBL343448

SMILES string:

C/C=C\1/C(=O)N[C@H](C(=O)O[C@H]\2CC(=O)N[C@@H](C(=O)N[C@H](CSSCC/C=C2)C(=O)N1)C(C)C)C(C)C

InChi Key:

OHRURASPPZQGQM-GCCNXGTGSA-N

Orthogonal probe:

RGFP966

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50

HDAC1: 36 nM, HDAC2: 47 nM

Potency assay:

In biochemical enzyme assays with synthetic substrates, FK-228 potently and selectively inhibited class I HDACs (IC50s, HDAC1: 0.0015 nM, HDAC2: 0.038 nM, HDAC3: 0.15 nM, HDAC8: 0.15 nM).

Off target activity

Potency (off target):

IC50

Off target protein and potency:

HDAC4: 510 nM, HDAC6: 14,000 nM

Potency assay (off target):

In biochemical assays with synthetic substrates, FK-228 was selective for class I HDACs (IC50s, HDAC4: 20.5 nM, HDAC5: 550 nM, HDAC6: 9.5 nM, HDAC7: 1.25 uM, HDAC9: 1.1 uM)

In cell validation

On target activity in cells

Potency in cells:

IC50

0.038 - 6.36 nM

Potency assay (cells):

In M-8 and HeLa cells, histone acetylation increased upon treatment with FK-228. Inhibition of cell viability in Hut-78 and Karpas-266 cell lines.

Primary Reference

Reference (doi):

10.1006/excr.1998.4027 Cancer Research 10.1038/nchembio.313

Reference (PMID):

9633520 12208741 20139990

Endorsed probe

The Chemical Probes Portal endorses this compound as chemical probe for use in cells and in model organisms.

SAB Rating

Rating for use in Cells

3 review(s)

Rating for use in Model Organisms

3 review(s)

SAB Members

SAB 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.

Jun 27 2017 - 1:53pm

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.

Jul 26 2017 - 1:20pm

Romidepsin

Probe Availability

Probe Information

Target Details

Histone deacetylase 1, GON-10, HD1, RPD3, RPD3L1, histone deacetylase 2, HD2, RPD3, YAF1, histone deacetylase 3, HD3, RPD3, RPD3-2, histone deacetylase 8, CDA07, CDLS5, HD8, HDACL1, MRXS6, RPD3, WTS, class I HDAC

Probe Details

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?

Search form

Romidepsin

Probe Availability

Probe Information

Target Details

Histone deacetylase 1, GON-10, HD1, RPD3, RPD3L1, histone deacetylase 2, HD2, RPD3, YAF1, histone deacetylase 3, HD3, RPD3, RPD3-2, histone deacetylase 8, CDA07, CDLS5, HD8, HDACL1, MRXS6, RPD3, WTS, class I HDAC

Probe Details

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?