XZ9002

XZ9002 : Degrader (PROTAC) of HDAC3

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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.

Probe XZ9002 is in the process of SERP review.

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Information

HDAC3

Degrader (PROTAC)

up to 200 nM

Probe Availability:

MedKoo

In Vitro Validations

Uniprot ID: O15379

Target Class: Epigenetic

Target SubClass: Histone deacetylase

Potency: IC50

Potency Value: 350 ± 70

Potency Assay: Enzymatic inhibition assay

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

Target aliases:

Histone deacetylase 3, HDAC3, HDAC3_HUMAN, HD3, SM ...

DOI Reference: 10.1039/D0CC03243C

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay, off target (cells): No significant changes in the protein levels of HDACs 1, 2, and 6 were observed under the same condition

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

This PROTAC does not achieve a high level of HDAC3 degradation (less than 80%). However, degradation is specific for HDAC3 versus HDAC1, 2 or 6. Overall selectivity has not been assessed as proteomics data are missing.

(last updated: 20 Feb 2025 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This PROTAC is not a selective degrader but pan-inhibitor (2-fold selectivity over HDAC1, 5-fold selectivity over HDAC2). Even though it potently degrades HDAC3, it may still have inhibitory effects on multiple HDAC iso-zymes. Moreover, it lacks wider proteomics profiling and therefore does not qualify as chemical probe.

(last updated: 6 Feb 2026 )