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Tubastatin-A | Tubastatin-A : Inhibitor of Class IIB HDACs HDAC6, HDAC10
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
HDAC6
  • IC 50:15 nM
  • IC 50:100 nM
HDAC10
  • IC 50:12.6 nM
  • IC 50:12.5 nM
Inhibitor
1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - HDAC8 854 nM

Potency Assay Off-Target:
Enzyme inhibition assays using the Reaction Biology HDAC Spectrum platform.
Selectivity Assessment Description:
Enzyme inhibition assays using the Reaction Biology HDAC Spectrum platform.

Potency
Cellular
In Vitro

HDAC6

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.8b01936

HDAC10

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.8b01936

In Vivo Validations

Mouse
Dose: 5 mg/Kg IV, 30 mg/Kg Oral
Route of delivery: Intravenous, Oral
Plasma half life: 0.35 h
Systemic clearance: 222 ml/min/Kg
Organ of interest (O): Kidney

DOI Reference: 10.1021/acs.jmedchem.8b01936

Orthogonal Probes def

5OJ
NEXTURASTAT A
SS-208

Chemical Information

Molecular Formula C20H21N3O2
SMILEs CN1CCc2c(c3ccccc3n2Cc2ccc(C(=O)NO)cc2)C1
InChI InChI=1S/C20H21N3O2/c1-22-11-10-19-17(13-22)16-4-2-3-5-18(16)23(19)12-14-6-8-15(9-7-14)20(24)21-25/h2-9,25H,10-13H2,1H3,(H,21,24)
Molecular weight 335.16 Da
AlogP 2.796500000000001
HBond acceptors 5
HBond donors 2
Atoms 46
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

References

Publications

Cross References

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 2 Jun 2020 )
Cellular Use Rating
In Model Organisms
This compound has been claimed to be HDAC6 selective except by DOI: 10.1021/acs.jmedchem.8b01936 where this compound was shown to be more active in HDAC10 by FRET and BRET (cellular) assays
by SERP
(on 28 Jun 2020 )
Cellular Use Rating
In Model Organisms
The biology of HDAC6 and HDAC10 are likely to be very different so, this probe should be used in combination with genetic knockdown and/or other more selective compounds for either HDAC6 or HDAC10 (see...

Portal Comments

Tubastatin A has been used in >100 publications to probe HDAC6 biology under the assumption of high HDAC6 selectivity but according to Lechner S et al 2022 paper (DOI:10.1038/s41589-022-01015-5), Tubastatin A...

(last updated: 25 May 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