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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

HPOB
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 )

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