General
Preferred name
QUISINOSTAT
Synonyms
Quisinostat (JNJ-26481585) 2HCl ()
JNJ26854165(Quisinostat) 2HCl ()
JNJ-26481585 2HCl ()
JNJ-26481585 ()
Quisinostat 2HCl ()
JNJ 26481585 dihydrochloride ()
JNJ-26481585 (dihydrochloride) ()
Quisinostat (dihydrochloride) ()
JNJ 26481585 ()
JNJ-26481585-AAC ()
Quisinostat hydrochloride ()
JNJ-26481585 (hydrochloride) ()
P&D ID
PD011142
CAS
875320-31-3
875320-29-9
Tags
available
obsolete probe
drug candidate
Drug indication
Solid tumour/cancer
Advanced stage follicular lymphoma
Drug Status
investigational
Max Phase
2.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Quisinostat is an HDAC inhibitor. The compound has highest potency for HDAC1 and modest potency with HDACs 2, 4, 10, and 11. Quisinostat exhibits >30-fold selectivity against HDACs 3, 5, 8, and 9, with lowest potency for HDACs 6 and 7 .
The compound also has antimalarial activity . The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. (GtoPdb)
The compound also has antimalarial activity . The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. (GtoPdb)
DESCRIPTION
Quisinostat, also known as JNJ-26481585, is an orally bioavailable, second-generation, hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor JNJ-26481585 inhibits HDAC leading to an accumulation of highly acetylated histones, which may result in an induction of chromatin remodeling; inhibition of the transcription of tumor suppressor genes; inhibition of tumor cell division; and the induction of tumor cell apoptosis. HDAC, an enzyme upregulated in many tumor types, deacetylates chromatin histone proteins. Compared to some first generation HDAC inhibitors, JNJ-26481585 may induce superior HSP70 upregulation and bcl-2 downregulation.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
JNJ 26481585 dihydrochloride is a potent and second-generation pan-HDAC inhibitor (IC50 value 0.11 nM for HDAC1, and sub-nanomolar for HDAC2, HDAC4, HDAC10, and HDAC11 in vitro) with antineoplastic activity. JNJ-26481585 inhibiting HDAC leads to continuous acetylation of histone H3, activation of the caspase cascade, upregulation of p21, and tumor cell apoptosis.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
3
Organisms
2
Compound Sets
16
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
Obsolete Compounds
ReFrame library
Selleckchem Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
43
Molecular Weight
394.21
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
3
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
3
cLogP
2.09
TPSA
95.31
Fraction CSP3
0.38
Chiral centers
0.0
Largest ring
6.0
QED
0.44
Structural alerts
1
historic compounds (Chemical Probes.org)
Obsolete
Related compounds
Custom attributes
(extracted from source data)
Pathway
Chromatin/Epigenetic
DNA Damage/DNA Repair
NF-??b
Apoptosis
Autophagy
Cell Cycle/DNA Damage
Epigenetics
Target
HDAC1
HDAC10
HDAC11
HDAC2
HDAC4
HDAC3
HDAC5
HDAC8
HDAC1, HDAC10, HDAC11, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9, MDM2
HDAC
MOA
HDAC inhibitor
Source data
