General
Preferred name
resminostat
Synonyms
4SC-201 ()
RAS2410 ()
4SC-201 hydrochloride ()
RAS2410 hydrochloride ()
Resminostat (RAS2410) ()
Resminostat (hydrochloride) ()
Resminostat hydrochloride ()
BYK408740 ()
RAS-2410 ()
BYK-408740 ()
P&D ID
PD010883
CAS
864814-88-0
1187075-34-8
Tags
available
drug candidate
nuisance
obsolete probe
Drug indication
Hepatocellular carcinoma
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
Resminostat hydrochloride is a potent inhibitor of HDAC1, HDAC3 and HDAC6, with mean IC50 values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities against HDAC8, with an IC50 of 877 nM.
PRICE
128
DESCRIPTION
Resminostat is an HDAC inhibitor with selectivity for HDACs 1, 3 and 6, with significantly lower affinity for HDAC8 .
(GtoPdb)
DESCRIPTION
Resminostat (RAS2410; 4SC-201) is a potent inhibitor of HDAC1, HDAC3 and HDAC6, with mean IC50 values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities against HDAC8, with an IC50 of 877 nM.
PRICE
130
DESCRIPTION
Resminostat is an inhibitor of histone deacetylase (HDAC) with IC50 values of 42.5nM, 50.1nM and 71.8nM, respectively against HDAC1, 3 and 6.
As an inhibitor of HDACs, resminostat also inhibits HDAC8 with a weak activity (IC50=877nM). 5μM resminostat induces the acetylation of histone H4 in U266 myeloma cells. 10μM resminostat completely suppresses the cell growth in human myeloma cell lines, such as OPM-2, RPMI-8226 and U266. This inhibition is proved to be caused by the induction of apoptosis. In primary myeloma cells, resminostat also induces apoptosis of cells. Besides that, resminostat is proved to downregulate the expression of cell cycle proteins, including phosphorylated Rb, cdc25a, cyclin D1, Cdk4 and p53. In addition, resminostat is reported to be well tolerated, have no unexpected toxicities and do not cause clinically significant myelosuppression in the first-human study. (BOC Sciences Bioactive Compounds)
As an inhibitor of HDACs, resminostat also inhibits HDAC8 with a weak activity (IC50=877nM). 5μM resminostat induces the acetylation of histone H4 in U266 myeloma cells. 10μM resminostat completely suppresses the cell growth in human myeloma cell lines, such as OPM-2, RPMI-8226 and U266. This inhibition is proved to be caused by the induction of apoptosis. In primary myeloma cells, resminostat also induces apoptosis of cells. Besides that, resminostat is proved to downregulate the expression of cell cycle proteins, including phosphorylated Rb, cdc25a, cyclin D1, Cdk4 and p53. In addition, resminostat is reported to be well tolerated, have no unexpected toxicities and do not cause clinically significant myelosuppression in the first-human study. (BOC Sciences Bioactive Compounds)
DESCRIPTION
Resminostat hydrochloride (RAS2410 hydrochloride) is an effective inhibitor of HDAC1/HDAC3/HDAC6 (IC50: 42.5/50.1/71.8 nM), respectively, and shows less potent activities against HDAC8 (IC50: 877 nM).
(TargetMol Bioactive Compound Library)
DESCRIPTION
Resminostat is an orally bioavailable inhibitor of histone deacetylases (HDACs) with potential antineoplastic activity. Resminostat binds to and inhibits HDACs leading to an accumulation of highly acetylated histones. This 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. HDACs, upregulated in many tumor types, are a class of enzymes that deacetylate chromatin histone proteins.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Resminostat (4SC-201) is an orally bioavailable inhibitor of histone deacetylases (HDACs) with potential antineoplastic activity.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
14
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
EUbOPEN Chemogenomics Library
Guide to Pharmacology
Nuisance compounds in cellular assays
Obsolete Compounds
ReFrame library
Selleckchem Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
32
Molecular Weight
349.11
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
2
Aromatic Ring Count
2
cLogP
1.31
TPSA
91.64
Fraction CSP3
0.19
Chiral centers
0.0
Largest ring
6.0
QED
0.47
Structural alerts
2
historic compounds (Chemical Probes.org)
Obsolete
Nonspecific HDAC inhibition
Nuisance compounds
Related compounds
Custom attributes
(extracted from source data)
Target
HDAC
HDAC1
HDAC3
HDAC6
HDAC8
HDAC1, HDAC3, HDAC6, HDAC8
MOA
HDAC inhibitor
Pathway
Chromatin/Epigenetic
DNA Damage/DNA Repair
Cell Cycle/DNA Damage
Epigenetics
Recommended Cell Concentration
1 uM
Source data
