Histone Deacetylases

Histone deacetylases (HDACs) are a group of enzymes closely related to sirtuins. They catalyze acetyl group removal from lysine residues in histones and non-histone proteins, causing transcriptional repression. HDACs are usually components of multiprotein complexes.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
4846 Apicidin
Potent histone deacetylase inhibitor
6010 BRD 4354
HDAC5 and HDAC9 inhibitor
6284 BRD 73954
Dual histone deacetylase (HDAC) 6/8 inhibitor
2952 CI 994
Class I histone deacetylase inhibitor; orally active
3515 FK 228
Potent and selective class I histone deacetylase inhibitor; antitumor
4830 LMK 235
Selective HDAC4/HDAC5 inhibitor
2771 M 344
Histone deacetylase inhibitor
4077 MC 1568
Selective HDAC class II (IIa) inhibitor
5727 MC 1742
Potent class I and IIb HDAC inhibitor
5647 MI 192
Potent and selective HDAC2/3 inhibitor
6208 MS 275
HDAC (Class I) inhibitor
3747 NCH 51
Histone deacetylase inhibitor
2521 NSC 3852
Histone deacetylase inhibitor
4643 PCI 34051
Potent and selective HDAC8 inhibitor
2682 Sodium 4-Phenylbutyrate
Histone deacetylase inhibitor
4403 Pyroxamide
Histone deacetylase inhibitor
4652 SAHA
Class I and II HDAC inhibitor
3810 SBHA
Histone deacetylase inhibitor
2421 Scriptaid
Histone deacetylase inhibitor
3850 Sodium butyrate
Histone deacetylase inhibitor
4270 TC-H 106
Class I histone deacetylase inhibitor
4805 TCS HDAC6 20b
Selective HDAC6 inhibitor
1406 Trichostatin A
Potent histone deacetylase inhibitor
3402 Tubacin
HDAC6 inhibitor; inhibits α-tubulin deacetylation
6270 Tubastatin A hydrochloride
Potent HDAC6 inhibitor
5588 UF 010
Class I HDAC inhibitor
2815 Valproic acid, sodium salt
Histone deacetylase inhibitor

Histone deacetylases (HDACs) are a group of enzymes closely related to sirtuins. They catalyze the removal of acetyl groups from lysine residues in histones and non-histone proteins, resulting in transcriptional repression. In general, they do not act autonomously but as components of large multiprotein complexes, such as pRb-E2F and mSin3A, that mediate important transcription regulatory pathways.

There are three classes of HDACs; classes 1, 2 and 4, which are closely related Zn2+-dependent enzymes. HDACs are ubiquitously expressed and they can exist in the nucleus or cytosol. Their subcellular localization is affected by protein-protein interactions (for example HDAC-14.3.3 complexes are retained in the cytosol) and by the class to which they belong (class 1 HDACs are predominantly nuclear whilst class 2 HDACs shuttle between the nucleus and cytosol). HDACs have a role in cell growth arrest, differentiation and death and this has led to substantial interest in HDAC inhibitors as possible antineoplastic agents.

Histone acetylation - a key epigenetic process - is upregulated during memory formation but downregulated in numerous neurodegenerative diseases, such as Alzheimer's disease and Huntington's disease. As a result, HDAC inhibitors are also of great interest in neuroscience research.

Literature for Histone Deacetylases

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

  • Alzheimer's disease
  • Parkinson's disease
  • Huntington's disease
Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
Depression

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

Histone Deacetylase Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
Class 1
HDAC1 Human HDAC1 NM_004964 Q13547
Mouse Hdac1 NM_008228 O09106
Rat Hdac1 NM_001025409 Q4QQW4
HDAC2 Human HDAC2 NM_001527 Q92769
Mouse Hdac2 NM_008229 P70288
Rat Hdac2 NM_053447 Q99PA1
HDAC3 Human HDAC3 NM_003883 O15379
Mouse Hdac3 NM_010411 O88895
Rat Hdac3 NM_053448 Q6P6W3
HDAC8 Human HDAC8 NM_018486 Q9BY41
Mouse Hdac8 NM_027382 Q8VH37
Rat Hdac8 NM_001126373 XP_343805
Class 2
HDAC4 Human HDAC4 NM_006037 P56524
Mouse Hdac4 NM_207225 Q6NZM9
Rat Hdac4 XM_343629 Q99P99
HDAC5 Human HDAC5 NM_001015053 Q9UQL6
Mouse Hdac5 NM_001077696 Q9Z2V6
Rat Hdac5 XM_001081495 Q5RJZ2
HDAC6 Human HDAC6 NM_006044 Q9UBN7
Mouse Hdac6 NM_010413 Q9Z2V5
Rat Hdac6 XM_228753 Q99P97
HDAC7 Human HDAC7 NM_016596 Q9UFU7
Mouse Hdac7 NM_019572 Q8C2B3
Rat Hdac7a XM_345868 Q99P96
HDAC9 Human HDAC9 NM_058177 Q9UKV0
Mouse Hdac9 NM_024124 Q99N13
HDAC10 Human HDAC10 NM_032019 Q969S8
Mouse Hdac10 NM_199198 Q6P3E7
Rat Hdac10 NM_001035000 Q569C4
Class 4
HDAC11 Human HDAC11 NM_024827 Q96DB2
Mouse Hdac11 NM_144919 Q91WA3
Rat Hdac11 NM_001106610 XP_238362