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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

References

Publications

Cross References

canSARChEMBLBindingDB

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 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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