General
Preferred name
AZ191
Synonyms
AZ 191 ()
CHEMBL3421968 ()
AZ-191 ()
P&D ID
PD003259
CAS
1594092-37-1
Tags
available
probe
Probe info
Probe type
calculated probe
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
2
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)
COMMENT
Concentrations higher than a few micromolar are likely to inhibit other kinases. Jun 11 2016 - 4:30am; AZ191 is claimed to have 5-10x selectivity over DYRK1A and >100x over DYRK2. This molecule has been tested against >400 kinases at 1 uM and only hits 9 of them. A range of cellular effects are reported as well as cellular markers of activity. This tool is recommended for use in preference to the older, less selective harmine and derivatives. Jun 11 2016 - 4:30am; This compound is too promiscuous kinome-wide to be useful as a cellular inhibitor of DYRK1B. Jun 30 2016 - 3:52am
DESCRIPTION
AZ191 is a potent and selective small molecule inhibitor of DYRK1B from AstraZeneca . Results of a 2014 study using AZ191 indicate DYRK1B is a novel Thr(286)-CCND1(cyclinD1) kinase that acts independently of GSK3β to regulate the mammalian G1-S-phase transition. This compound is included in the Probe Portal as SGC AZ191. It was tested in preclinical studies.
(GtoPdb)
DESCRIPTION
AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM[1].
PRICE
82
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
Rho/SRF pathway inhibitor; induces intermediate mesoderm differentiation from ESCs
(Tocris Bioactive Compound Library)
DESCRIPTION
Potent DYRK1B inhibitor
(Tocriscreen Plus)
DESCRIPTION
AZ191 is a cell-permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50 = 17 nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
AZ191(IC50 of 17 nM) is an effective and specific DYRK1B inhibitor. The specificity of AZ191 for DYRK1B is about 5- and 110-fold greater over DYRK1A and DYRK2, respectively.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
1
Compound Sets
18
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
Chemical Probes.org
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
JUMP-MOA Compound Set
JUMP-Target 1 Compound Set
Kinase Inhibitors (best-in-class)
MedChem Express Bioactive Compound Library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Tool Compound Set
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
13
Molecular Weight
429.23
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
4
cLogP
3.53
TPSA
71.34
Fraction CSP3
0.29
Chiral centers
0.0
Largest ring
6.0
QED
0.52
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
DYRK
DYRK1B
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
DYRK1A
DYRK2
Target Type
Enzymes
Kinase group
CMGC
MOA
Inhibitor
DYRK inhibitor
Pathway
Protein Tyrosine Kinase/RTK
Cell Cycle/Checkpoint
Tyrosine Kinase/Adaptors
Target class
Protein kinase
Recommended Cell Concentration
1 uM
Source data
