TH65

TH65 : Inhibitor of HDAC10

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe TH65 is in the process of SERP review.

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Information

HDAC10

Inhibitor

up to 5 uM

In Vitro Validations

Uniprot ID: Q969S8

Target Class: Epigenetic

Target SubClass: Histone Deacetylase

Potency: Kd

Potency Value: 630 nM

Potency Assay: chemical proteomics

PDB ID for probe-target interaction (3D structure): 6HTH

Target aliases:

Polyamine deacetylase HDAC10, HDAC10, HDA10_HUMAN, ...

DOI Reference: 10.1038/s41589-022-01015-5

Uniprot ID: Q969S8

Target Class: Epigenetic

Target SubClass: Histone Deacetylase

Potency: IC50

Potency Value: 100 nM

Potency Assay: FRET

PDB ID for probe-target interaction (3D structure): 6HTH

Target aliases:

Polyamine deacetylase HDAC10, HDAC10, HDA10_HUMAN, ...

DOI Reference: 10.1038/s41589-022-01015-5

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Concentration- And Target-Dependent Selectivity (CATDS) score shows high selectivity for HDAC10 within HADC family.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

TH65 was recently discovered as a selective HDAC10 binder in a chemoproteomics study. Interestingly, TH65 was originally developed and promoted as a selective HDAC8 inhibitor, potent against both the S. mansoni, but also the human subtype. As the chemoproteomics data appears to be inconsistent with this data, caution should be taken when considering this compound as an HDAC10 chemical probe. Independent measurement of cellular HDAC8 binding (e.g. BRET assay) would be highly valuable.

(last updated: 4 Jul 2022 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

TH65 shows sufficient potency (600 nM), especially compared to the activities against other HDACs (higher than 30 uM). This is the most selective compound to date with only one off-target, which is however unrelated to the HDAC family. Several assays have proven the binding affinity lower than 1 uM. The in vivo assay was performed on Mesocestoides vogae. No solubility, toxicity or stability issues were reported.

(last updated: 17 Jun 2024 )