General
Preferred name
GSK583
Synonyms
GSK 583 ()
GSK-583 ()
GTPL9134 ()
SCHEMBL2595766 ()
GSK'583 ()
CS-5543 ()
HY-100339 ()
P&D ID
PD049179
CAS
1346547-00-9
Tags
available
probe
Probe info
Probe type
P&D approved
experimental probe
Probe selectivity
protein-selective
Probe sources
Chemical Probes.org
High-quality chemical probes
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 GSK583 is a potent and selective molecule for the inhibition of RIP2 kinase, and it could be useful in probing the role of NOD1 and NOD2 in the pathogenesis of inflammatory disease. The compound has a reasonable profile for in vivo studies in rodents but falls short for human studies due to low exposure and safety concerns related to both hERG and CYP3A4. Mar 29 2017 - 11:59am
DESCRIPTION GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 inhibits both TNF-¦Á and IL-6 production with an IC50 value of 200 nM.
PRICE 167
DESCRIPTION GSK583 is a potent and selective next generation inhibitor of receptor interacting serine/threonine kinase 2 (RIP2 kinase) . It is compound 27 in and compound 89 claimed in patent WO2011140442 . GSK583 can be used as a tool compound to investigate the role played by RIP2 kinase in NOD1 and NOD2 mediated pathology. (GtoPdb)
MOA Inhibitor (Chemical Probes.org)
DESCRIPTION GSK583 is a highly effective and specific RIP2 kinase inhibitor (IC50: 5 nM). (TargetMol Bioactive Compound Library)
DESCRIPTION Potent and selective MST1/2 inhibitor; orally bioavailable (Tocris Bioactive Compound Library)
Cell lines
1
Organisms
2
Compound Sets
15
Cayman Chemical Bioactives
19739
Chemical Probes.org
gsk583
Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors
CZ-OPENSCREEN Bioactive Library
EU-OPENSCREEN Bioactive Compound Library
EOS101451
EUbOPEN Chemogenomics Library
EUB0001882
Guide to Pharmacology
9134
High-quality chemical probes
PD049179
Kinase Chemogenomic Set (KCGS)
GSK583
Mcule NIBR MoA Box Subset
MCULE-4905690608
MedChem Express Bioactive Compound Library
HY-100339
Novartis Chemogenetic Library (NIBR MoA Box)
Selleckchem Bioactive Compound Library
gsk583
TargetMol Bioactive Compound Library
T3537
Tocris Bioactive Compound Library
6480
External IDs
15
Properties
(calculated by RDKit )
Molecular Weight
398.12
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
3
Ring Count
4
Aromatic Ring Count
4
cLogP
4.57
TPSA
87.74
Fraction CSP3
0.2
Chiral centers
0.0
Largest ring
6.0
QED
0.53
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Pathway
Apoptosis
NF-κB
Primary Target
Receptor Interacting Protein Kinases
MOA
Inhibitor
RIPK2 inhibitor
Target
RIPK2
NF-??
Interleukins,RIP kinase,TNF-alpha
RIP Kinase
RIP1
RIP3
Member status
member
Target class
Protein kinase
Kinase
Target subclass
TKL
Recommended Cell Concentration
100 nM
Source data