histone deacetylase 9

Target id: 2620

Nomenclature: histone deacetylase 9

Family: 3.5.1.- Histone deacetylases (HDACs)

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for histone deacetylase 9 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1011 7p21.1 HDAC9 histone deacetylase 9
Mouse - 588 12 A3 Hdac9 histone deacetylase 9
Rat - 1068 6q16 Hdac9 histone deacetylase 9
Previous and Unofficial Names
HD7 | HDAC7B | MITR
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.5.1.98

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
vorinostat Hs Inhibition 7.2 pKi 6
pKi 7.2 (Ki 6.5x10-8 M) [6]
belinostat Hs Inhibition 6.6 pKi 2
pKi 6.6 (Ki 2.5x10-7 M) [2]
givinostat Hs Inhibition 6.4 pKi 2
pKi 6.4 (Ki 3.9x10-7 M) [2]
trichostatin A Hs Inhibition 6.1 pKi 2
pKi 6.1 (Ki 8x10-7 M) [2]
romidepsin Hs Inhibition 6.0 pKi 2
pKi 6.0 (Ki 1.1x10-6 M) [2]
scriptaid Hs Inhibition 5.1 pKi 2
pKi 5.1 (Ki 8x10-6 M) [2]
dacinostat Hs Inhibition 5.1 pKi 2
pKi 5.1 (Ki 9x10-6 M) [2]
panobinostat Hs Inhibition 8.5 pEC50 4
pEC50 8.5 (EC50 3x10-9 M) [4]
belinostat Hs Inhibition 6.9 pEC50 4
pEC50 6.9 (EC50 1.28x10-7 M) [4]
entinostat Hs Inhibition 6.3 pEC50 4
pEC50 6.3 (EC50 5.05x10-7 M) [4]
TMP269 Hs Inhibition 7.6 pIC50 5
pIC50 7.6 (IC50 2.3x10-8 M) [5]
quisinostat Hs Inhibition 7.5 pIC50 1
pIC50 7.5 (IC50 3.21x10-8 M) [1]
CUDC-101 Hs Inhibition 7.2 pIC50 3
pIC50 7.2 (IC50 6.72x10-8 M) [3]
Inhibitor Comments
Vorinostat has high affinity for HDACs 2, 3, 6, 9, 10 and 11, but 10-fold lower affinity for HDAC8
Clinically-Relevant Mutations and Pathophysiology
Disease:  Peters anomaly
Orphanet: ORPHA708
General Comments
HDAC9 is a Class II histone deacetylase.

References

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1. Arts J, King P, Mariën A, Floren W, Beliën A, Janssen L, Pilatte I, Roux B, Decrane L, Gilissen R et al.. (2009) JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin. Cancer Res.15 (22): 6841-51. [PMID:19861438]

2. Bradner JE, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T, Mazitschek R. (2010) Chemical phylogenetics of histone deacetylases. Nat. Chem. Biol.6 (3): 238-243. [PMID:20139990]

3. Cai X, Zhai HX, Wang J, Forrester J, Qu H, Yin L, Lai CJ, Bao R, Qian C. (2010) Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer. J. Med. Chem.53 (5): 2000-9. [PMID:20143778]

4. Khan N, Jeffers M, Kumar S, Hackett C, Boldog F, Khramtsov N, Qian X, Mills E, Berghs SC, Carey N et al.. (2008) Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. Biochem. J.409 (2): 581-9. [PMID:17868033]

5. Lobera M, Madauss KP, Pohlhaus DT, Wright QG, Trocha M, Schmidt DR, Baloglu E, Trump RP, Head MS, Hofmann GA et al.. (2013) Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group. Nat. Chem. Biol.9 (5): 319-25. [PMID:23524983]

6. Wang H, Lim ZY, Zhou Y, Ng M, Lu T, Lee K, Sangthongpitag K, Goh KC, Wang X, Wu X et al.. (2010) Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity. Bioorg. Med. Chem. Lett.20 (11): 3314-21. [PMID:20451378]

How to cite this page

3.5.1.- Histone deacetylases (HDACs): histone deacetylase 9. Last modified on 27/10/2015. Accessed on 18/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2620.