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
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 7
pKi 7.2 (Ki 6.5x10-8 M) [7]
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 5
pEC50 8.5 (EC50 3x10-9 M) [5]
belinostat Hs Inhibition 6.9 pEC50 5
pEC50 6.9 (EC50 1.28x10-7 M) [5]
entinostat Hs Inhibition 6.3 pEC50 5
pEC50 6.3 (EC50 5.05x10-7 M) [5]
TMP269 Hs Inhibition 7.6 pIC50 6
pIC50 7.6 (IC50 2.3x10-8 M) [6]
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]
KA1010 Hs Inhibition 6.3 pIC50 4
pIC50 6.3 (IC50 5.58x10-7 M) [4]
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. Ellis JD, Neil DA, Inston NG, Jenkinson E, Drayson MT, Hampson P, Shuttleworth SJ, Ready AR, Cobbold M. (2016) Inhibition of Histone Deacetylase 6 Reveals a Potent Immunosuppressant Effect in Models of Transplantation. Transplantation, 100 (8): 1667-74. [PMID:27222932]

5. 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]

6. 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]

7. 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 25/09/2017. Accessed on 15/07/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2620.