General
Preferred name
GSK-J1
Synonyms
GSK J1 ()
GSK-J1 sodium salt ()
GSK-J1 (sodium salt) ()
P&D ID
PD012892
CAS
1373422-53-7
1797832-71-3
Tags
available
probe
drug candidate
obsolete probe
Drug indication
Discovery agent
Probe info
Probe type
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Orthogonal probes
1
No orthogonal probes found
Similar probes
1
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
GSK-J1 is a catalytic site inhibitor that is somewhat selective for the H3K27me3-specific demethylases KDM6A and 6B (a.k.a. UTX and JMJD3 respectively) . The compund has also been shown to inhibit H3K4me3/me2 catalysed by KDM5 enzymes in vitro .
This is a compound from the Structural Genomics Consortium's (SGC) Epigenetics Probes Collection. It reduces lipopolysaccharide-induced proinflammatory cytokine production by human primary macrophages, a process that depends on both JMJD3 and UTX. (GtoPdb)
This is a compound from the Structural Genomics Consortium's (SGC) Epigenetics Probes Collection. It reduces lipopolysaccharide-induced proinflammatory cytokine production by human primary macrophages, a process that depends on both JMJD3 and UTX. (GtoPdb)
DESCRIPTION
GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
PRICE
52
DESCRIPTION
Potent JMJD3/UTX inhibitor
(Tocriscreen Plus)
DESCRIPTION
Histone KDM inhibitor; cell permeable
(Tocris Bioactive Compound Library)
DESCRIPTION
GSK-J1 is an inhibitor of histone lysine demethylases with IC50s of lysine-specific demethylase 6A, lysine-specific demethylase 5A and lysine-specific demethylase 5B with IC50s of 2.2, 5.3 and 6 µM.
(Enamine Bioactive Compounds)
DESCRIPTION
GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases.
(TargetMol Bioactive Compound Library)
DESCRIPTION
GSK-J1 is a potent and selective inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50s = 18 and 56 µM, respectively; IC50 = 60 nM in JMJD3 antibody-based assays).
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
4
Organisms
0
Compound Sets
19
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
Enamine Bioactive Compounds
Enamine BioReference Compounds
EUbOPEN Chemogenomics Library
Guide to Pharmacology
LINCS compound set
MedChem Express Bioactive Compound Library
Obsolete Compounds
Selleckchem Bioactive Compound Library
SGC Probes
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
30
Molecular Weight
389.19
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
3
cLogP
3.03
TPSA
91.24
Fraction CSP3
0.27
Chiral centers
0.0
Largest ring
7.0
QED
0.67
Structural alerts
1
historic compounds (Chemical Probes.org)
Obsolete
Related compounds
Custom attributes
(extracted from source data)
Target Type
Enzymes
Target
Histone Demethylase
JMJD3 (KDM6B)
UTX (KDM6A)
KDM6B
JMJD3/UTX inhibitor
Histone Demethylase,JMJD
KDM6A
KDM5B
Primary Target
Histone Demethylases
MOA
Inhibitor
Histone Demethylase inhibitor
Pathway
Epigenetics
Chromatin/Epigenetic
Protein Family
KDM
Recommended Cell Concentration
100 nM
Source data
