General
Preferred name
DACINOSTAT
Synonyms
LAQ824 ()
Dacinostat, NVP-LAQ824 ()
LAQ824 (NVP-LAQ824) ()
NVP-LAQ824 ()
LAQ824 (NVP-LAQ824, Dacinostat) ()
Dacinostat (LAQ824) ()
Laq-824 ()
P&D ID
PD011143
CAS
404951-53-7
Tags
available
drug candidate
obsolete probe
Drug indication
leukaemia
Mood disorder
Multiple myeloma
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 formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
NVP-LAQ824 is a non-selective histone deacetylase (HDAC) inhibitor.
(GtoPdb)
DESCRIPTION
Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.
PRICE
151
DESCRIPTION
LAQ824 (Dacinostat (NVP-LAQ824)) is a novel HDAC inhibitor with IC50 of 32 nM and is an activator of the p21 promoter.
DESCRIPTION
Dacinostat, also known as LAQ824, is a hydroxamate histone deacetylase inhibitor with potential anticancer activity. LAQ824 sensitized nonsmall cell lung cancer to the cytotoxic effects of ionizing radiation. LAQ824 reduced clonogenic survival of the H23 and H460 cell lines five-fold compared with controls and four-fold compared with either agent alone (P<0.001). In phase I trials, LAQ824 was well tolerated at doses that induced accumulation of histone acetylation, with higher doses inducing changes consistent with HSP90 inhibition.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
56
Organisms
1
Compound Sets
14
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
Guide to Pharmacology
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
Obsolete Compounds
ReFrame library
Selleckchem Bioactive Compound Library
Welcome Trust Cancer Drugs
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
25
Molecular Weight
379.19
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
4
Rotatable Bonds
9
Ring Count
3
Aromatic Ring Count
3
cLogP
2.72
TPSA
88.59
Fraction CSP3
0.23
Chiral centers
0.0
Largest ring
6.0
QED
0.26
Structural alerts
1
historic compounds (Chemical Probes.org)
Obsolete
Custom attributes
(extracted from source data)
Pathway
chromain histone acetylation
Chromatin/Epigenetic
DNA Damage/DNA Repair
NF-¦ªb
Cell Cycle/DNA Damage
Epigenetics
Target
HDAC
HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9
Autophagy
HDAC,p21
Member status
member
MOA
HDAC 1/2/3/6/8/10/11
Antimitotic Drugs
Apoptosis Inducers
Histone Deacetylase (HDAC) Inhibitors
HDAC inhibitor
Source data

