Tubastatin-A
Tubastatin-A : Inhibitor of Class IIB HDACs HDAC6, HDAC10
Structure
In Cells
In Model Organisms
Probe Tubastatin-A is in the process of SERP review.
Please continue to check back for new reviews and commentary.
SERP ratings and comments
SERP Ratings
SERP Comments:
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
(last updated: 2 Jun 2020 )
SERP Ratings
SERP Comments:
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 for example Geraldy et al J. Med. Chem. 2019, 62, 9, 4426–4443) in order to attribute affects of Tubistatin A to one of these enzymes.
(last updated: 28 Jun 2020 )
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 has a much higher potency for HDAC10 than HDAC6 (pKdapp, HDAC10 = 7.5 vs pKdapp, HDAC6 = 5.0). Additionally, metallo-β-lactamase domain-containing protein 2 (MBLAC2) as additional off-target for Tubastatin A with an affinity of below 1 µM.
(last updated: 25 May 2022)