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histone deacetylase 9

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Target not currently curated in GtoImmuPdb

Target id: 2620

Nomenclature: histone deacetylase 9

Family: 3.5.1.- Histone deacetylases (HDACs)

Contents:

Gene and Protein Information Click here for help
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 Click here for help
HD7 | HDAC7B | MITR
Database Links Click here for help
Alphafold Q9UKV0 (Hs), Q99N13 (Mm)
BRENDA 3.5.1.98
CATH/Gene3D 3.40.800.20
ChEMBL Target CHEMBL4145 (Hs)
DrugBank Target Q9UKV0 (Hs)
Ensembl Gene ENSG00000048052 (Hs), ENSMUSG00000004698 (Mm), ENSRNOG00000004158 (Rn)
Entrez Gene 9734 (Hs), 79221 (Mm), 687001 (Rn)
Human Protein Atlas ENSG00000048052 (Hs)
KEGG Enzyme 3.5.1.98
KEGG Gene hsa:9734 (Hs), mmu:79221 (Mm), rno:687001 (Rn)
OMIM 606543 (Hs)
Orphanet ORPHA122391 (Hs)
Pharos Q9UKV0 (Hs)
RefSeq Nucleotide NM_058176 (Hs), NM_001271386 (Mm), NM_001200045 (Rn)
RefSeq Protein NP_478056 (Hs), NP_001258315 (Mm), NP_001186974 (Rn)
UniProtKB Q9UKV0 (Hs), Q99N13 (Mm)
Wikipedia HDAC9 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.5.1.98

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
vorinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pKi 7
⤷ pKi 7.2 (Ki 6.5x10-8 M) [7]
belinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pKi 2
⤷ pKi 6.6 (Ki 2.5x10-7 M) [2]
givinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.4 pKi 2
⤷ pKi 6.4 (Ki 3.9x10-7 M) [2]
trichostatin A Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.1 pKi 2
⤷ pKi 6.1 (Ki 8x10-7 M) [2]
romidepsin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 6.0 pKi 2
⤷ pKi 6.0 (Ki 1.1x10-6 M) [2]
scriptaid Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.1 pKi 2
⤷ pKi 5.1 (Ki 8x10-6 M) [2]
dacinostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.1 pKi 2
⤷ pKi 5.1 (Ki 9x10-6 M) [2]
panobinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Guide to Malaria Pharmacology Ligand Hs Inhibition 8.5 pEC50 5
⤷ pEC50 8.5 (EC50 3x10-9 M) [5]
belinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.9 pEC50 5
⤷ pEC50 6.9 (EC50 1.28x10-7 M) [5]
entinostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pEC50 5
⤷ pEC50 6.3 (EC50 5.05x10-7 M) [5]
TMP269 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 pIC50 6
⤷ pIC50 7.6 (IC50 2.3x10-8 M) [6]
quisinostat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Guide to Malaria Pharmacology Ligand Hs Inhibition 7.5 pIC50 1
⤷ pIC50 7.5 (IC50 3.21x10-8 M) [1]
CUDC-101 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 3
⤷ pIC50 7.2 (IC50 6.72x10-8 M) [3]
KA1010 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand 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
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  B cell (activation)
Immuno Process:  Immune system development
Immuno Process:  Cellular signalling
Immuno Process:  Cytokine production & signalling
Clinically-Relevant Mutations and Pathophysiology Click here for help
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 07/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2620.