Tubacin | Tubacin : Reversible inhibitor of HDAC6
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 reviews)
In Vivo

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
HDAC6
  • Ki:0.016 uM
  • EC50:2.5 uM
Inhibitor
Up to 200 nM

Selectivity

In Vitro Selectivity Assessment

Potency: Ki - HDAC1: 0.028 uM, HDAC2: 0.042 uM, HDAC3: 0.275 uM, HDAC4: 17 uM, HDAC5: 1.5 uM, HDAC7: 8.5 uM, HDAC8: 0.17 uM

In Cell Selectivity Assessment
Potency Assay Off-Target:
Tubacin had no affect on cellular morphology (microtubules) in A549 cells. Tubacin did not lead to c ...

Potency
Cellular
In Vitro

HDAC6

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Negative Control Compounds

NILTUBACIN

Orthogonal Probes def

TUBASTATIN A
SS-208
ACY-738

Chemical Information

Molecular Formula C41H43N3O7S
SMILEs O=C(CCCCCCC(=O)Nc1ccc([C@@H]2O[C@H](c3ccc(CO)cc3)C[C@H](CSc3nc(-c4ccccc4)c(-c4ccccc4)o3)O2)cc1)NO
InChI InChI=1S/C41H43N3O7S/c45-26-28-17-19-29(20-18-28)35-25-34(27-52-41-43-38(30-11-5-3-6-12-30)39(51-41)31-13-7-4-8-14-31)49-40(50-35)32-21-23-33(24-22-32)42-36(46)15-9-1-2-10-16-37(47)44-48/h3-8,11-14,17-24,34-35,40,45,48H,1-2,9-10,15-16,25-27H2,(H,42,46)(H,44,47)/t34-,35+,40+/m1/s1
Molecular weight 721.28 Da
AlogP 6.6796
HBond acceptors 10
HBond donors 4
Atoms 95

References

Publications

    Cross References

    canSARChEMBLBindingDB

    Vendors

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    Expert Reviews


    (on 28 Apr 2017 )
    Cellular Use Rating
    In Model Organisms
    Tubacin (tubulin acetylation inducer) is a small molecule that inhibits histone deacetylase 6 (HDAC6) and induces acetylation of α-tubulin. The use of Tubacin in models of disease has helped to validate,...
    (on 11 May 2017 )
    Cellular Use Rating
    In Model Organisms
    Even though tubacin was the first HDAC6 inhibitor identified that targets tubulin acetylation 14 years ago, it remains of great interest, particularly as an antitumor and neuroprotective agent. It is...
    (on 22 Jun 2017 )
    Cellular Use Rating
    ( The reviewer did not leave any comments )

    Portal Comments

    Tubacin and several other HDAC inhibitors have been independently profiled using a proteomics approach (Lechner et al). They identified metallo-β-lactamase domain-containing protein 2 (MBLAC2) as additional...

    (last updated: 8 Jun 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