General
Preferred name
UNC0638
Synonyms
UNC 0638 ()
UNC-0638 ()
UNC0638 hydrate ()
P&D ID
PD000003
CAS
1255580-76-7
1255517-77-1
Tags
available
probe
drug candidate
Drug indication
Discovery agent
Probe info
Probe type
calculated probe
experimental probe
Probe sources
Chemical Probes.org
High-quality chemical probes
Nature Chemical Biology Probes
SGC Probes
Tool Compound Set
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
COMMENT I recommend using UNC0638 in parallel with A-366 (as an orthogonal control). Jun 16 2016 - 5:46pm; The compound shows inhibitory activity against a few GPCR receptors such as M2, alpha1a and alpha1b at 1 micromolar in vitro, while it is not clear if there is such effect in vivo. So, when you use the compound in animal models, you need to carefully examine the effect of the probe, especially if you use the compound in neurology purpose. Nov 10 2020 - 12:40pm
MOA protein substrate competitive inhibitor;SAM noncompetitive inhibitor
DESCRIPTION This is a compound from the Structural Genomics Consortium's (SGC) Epigenetics Probes Collection. (GtoPdb)
DESCRIPTION UNC0638 selectively inhibits G9a and GLP histone methyltransferases with IC50 of 15 nM and 19 nM, respectively. UNC0638 inhibits TNBC cell invasion and migration in vitro. UNC0638 is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets[1][2][3][4][5].
PRICE 81
DESCRIPTION UNC0638 is an inhibitor of ??-protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.
MOA Inhibitor (Chemical Probes.org)
DESCRIPTION inhibitor of EHMT2 and GLP methyltransferase (Informer Set)
DESCRIPTION Selective G9a and GLP inhibitor (Tocriscreen Plus)
DESCRIPTION Potent VEGFR-1, -2 and -3 inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION UNC 0638 is a selective inhibitor of G9a/EHMT2 and GLP histone lysine methyltransferases (IC50 values are < 15 nM and 19 nM for G9a and GLP respectively, and > 10000 nM for a panel of other histone methyltransferases). UNC 0638 inhibits dimethylation of H3K9 in MCF-7 cells (IC50 = 70 nM). (BOC Sciences Bioactive Compounds)
DESCRIPTION UNC0638 is an inhibitor of β-protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets. (TargetMol Bioactive Compound Library)
Cell lines
43
Organisms
1
Compound Sets
26
AdooQ Bioactive Compound Library
A12947
A13690
Axon Medchem Screening Library
1889
BOC Sciences Bioactive Compounds
unc0638-hydrate-cas-1255517-77-1-170518
Cayman Chemical Bioactives
10734
Chemical Probes.org
unc0638
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
DM4A1KJ
EU-OPENSCREEN Bioactive Compound Library
EOS101593
EUbOPEN Chemogenomics Library
EUB0001125
Guide to Pharmacology
7015
High-quality chemical probes
PD000003
Informer Set
594665
IPPI - DB
2317
LINCS compound set
10320-101
MedChem Express Bioactive Compound Library
HY-15273
Nature Chemical Biology Probes
599
Novartis Chemogenetic Library (NIBR MoA Box)
Other bioactive compounds
Selleckchem Bioactive Compound Library
unc0638
SGC Probes
UNC0638
TargetMol Bioactive Compound Library
T3257
Tocris Bioactive Compound Library
4343
Tocriscreen Plus
4343
Tool Compound Set
Welcome Trust Cancer Drugs
1236
245
External IDs
26
Properties
(calculated by RDKit )
Molecular Weight
509.37
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
1
Rotatable Bonds
10
Ring Count
5
Aromatic Ring Count
2
cLogP
5.84
TPSA
62.75
Fraction CSP3
0.73
Chiral centers
0.0
Largest ring
6.0
QED
0.4
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
EHMT1
EHMT2
G9a(EHMT2), GLP(EHMT1)
Histone-lysine N-methyltransferase, H3 lysine-9 specific 3
Histone-lysine N-methyltransferase, H3 lysine-9 specific 5
EHMT1, EHMT2
G9a HMTase inhibitor
Histone methyltransferase
Influenza Virus
VSV
Antiviral,G9a/GLP,Histone Methyltransferase
EHMT2, EHMT1
Compound status
probe
Target Type
Enzymes
Pathway
chromatin histone methylation
Autophagy
Chromatin/Epigenetic
Microbiology/virology
Anti-infection
Primary Target
G9a/GLP
MOA
Inhibitor
EHMT1/2
Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (EHMT2| G9a) Inhibitors
histone lysine methyltransferase inhibitor
Member status
member
Target subclass
Protein methyltransferase
Protein methyltransferase, Protein methyltransferase
Target class
Epigenetics
Epigenetic, Epigenetic
Orthogonal probe
A-366
Protein Family
Histone Methyltransferase
Control
QQS
Recommended Cell Concentration
1 uM
Source data