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Romidepsin | Romidepsin : Non-covalent nhibitor of HDAC1, HDAC2, HDAC3, HDAC8
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
HDAC1
  • IC50:36 nM
  • Ki:0.015
  • IC50:0.038 - 6.36 nM
HDAC2
  • IC50:47 nM
  • Ki:0.038 nM
  • IC50:0.038 - 6.36 nM
HDAC3
  • Ki:0.15 nM
  • IC50:0.038 - 6.36 nM
HDAC8
  • Ki:0.15 nM
  • IC50:0.038 - 6.36 nM
Inhibitor
1-100 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - 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, HDAC ...

Potency
Cellular
In Vitro

HDAC1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.313

HDAC2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.313

HDAC3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.313

HDAC8

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.313

Orthogonal Probes def

RGFP966

Chemical Information

Molecular Formula C24H36N4O6S2
SMILEs C/C=C1\NC(=O)[C@H]2CSSCC/C=C/[C@H](CC(=O)N[C@H](C(C)C)C(=O)N2)OC(=O)[C@H](C(C)C)NC1=O
InChI InChI=1S/C24H36N4O6S2/c1-6-16-21(30)28-20(14(4)5)24(33)34-15-9-7-8-10-35-36-12-17(22(31)25-16)26-23(32)19(13(2)3)27-18(29)11-15/h6-7,9,13-15,17,19-20H,8,10-12H2,1-5H3,(H,25,31)(H,26,32)(H,27,29)(H,28,30)/b9-7+,16-6-/t15-,17-,19-,20+/m1/s1
Molecular weight 540.21 Da
AlogP 1.4296
HBond acceptors 10
HBond donors 4
Atoms 72

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 public comments)
by SERP
(on 27 Jun 2017)
Cellular Use Rating
In Model Organisms
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...
by SERP
(on 18 Jul 2017)
Cellular Use Rating
In Model Organisms
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.
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