Tubacin

Selective, Reversible Inhibitor of HDAC6

Structure

Information

Protein target names: HDAC6

Mechanism of action: Selective, Reversible Inhibitor

In Vitro Validations

Uniprot ID: Q9UBN7
Target Class: Epigenetics
Target SubClass: HDAC
Potency: Ki
Potency Value: 0.016 uM
Potency Assay: Biochemical enzyme assay with synthetic substrates (see Nature Chemical Biology paper)
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Histone deacetylase 6, KIAA0901, HDAC6, HDAC6_HUMA ...

In Cell Validations

In Vivo Data

No in Vivo Validations

Reagent authentication certificate: PDF image

SERP ratings and comments


28 Apr 2017

SERP Ratings

In Cell Rating
In Model Organisms
Comments:

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, in part, HDAC6 as a drug target, but its non-drug-like structure, high lipophilicity conspire to make it more useful as a research tool than a drug. Tubacin was found to potently inhibit HDAC6, with an IC50 value of 4 nM and approximately 350-fold selectivity over HDAC1. Tubacin induced alpha-tubulin hyperacetylation at ~2.5 to 10 μM concentrations.

11 May 2017

SERP Ratings

In Cell Rating
In Model Organisms
Comments:

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 a potent, selective HDAC6 inhibitor. Tubacin was found to inhibit the deacetylation of alpha-tubulin in mammalian cells without affecting histone acetylation, gene expression or cell-cycle progression. An interesting feature of tubacin is the lack of toxicity for normal haematological cells. As a result of its non drug-like structure (MW= 721, PSA 139, ClogP 4.85, 4 HBD, rotatable bonds > 10), tubacin is administered intraperitoneally and is more a useful research tool than a drug.