General
Preferred name
STAUROSPORINE
Synonyms
AM-2282 ()
STS ()
Antibiotic AM-2282 ()
Antibiotic AM-2282, STS ()
Staurosporine (AM-2282) ()
P&D ID
PD003511
CAS
109189-95-9
62996-74-1
Tags
nuisance
drug candidate
obsolete probe
covalent binder
natural product
available
Drug indication
Discovery agent
Drug Status
experimental
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine also inhibits TAOK2 with an IC50 of 3 ¦ÌM. Staurosporine is an apoptosis inducer[1][2][3][4][5].
DESCRIPTION Staurosporine is a non-specific, ATP-competitive inhibitor of protein kinase C (PKC) isolated from a Streptomyces strain . It inhibits all PKC enzyme isoforms , but has a more potent inhibitory effect on PKCs associated with the cell membrane compared to cytosolic PKCs.
Staurosporine analogues such as and are being investigated as therapeutics. (GtoPdb)
DESCRIPTION inhibitor of multiple kinases (Informer Set)
Cell lines
71
Organisms
5
Compound Sets
18
A Collection of Useful Nuisance Compounds (CONS) for Interrogation of Bioassay Integrity
AdooQ Bioactive Compound Library
A10864
Cayman Chemical Bioactives
81590
CovalentInDB
CI000044
CZ-OPENSCREEN Bioactive Library
DrugBank
DB02010
DrugMAP
DM0E9BR
Guide to Pharmacology
346
Informer Set
50769
LINCS compound set
10103-999
10103-101
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL388978
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL388978
MedChem Express Bioactive Compound Library
HY-15141
Novartis Chemogenetic Library (NIBR MoA Box)
Nuisance compounds in cellular assays
Obsolete Compounds
staurosporine
Reference compounds for characterizing cellular injury in high-content cellular morphology assays
Selleckchem Bioactive Compound Library
Staurosporine
External IDs
34
Properties
(calculated by RDKit )
Molecular Weight
466.2
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
2
Ring Count
8
Aromatic Ring Count
5
cLogP
4.35
TPSA
69.45
Fraction CSP3
0.32
Chiral centers
4.0
Largest ring
7.0
QED
0.41
Structural alerts
2
historic compounds (Chemical Probes.org)
Obsolete
Nonspecific kinase inhibition
Nuisance compounds
Related compounds
Custom attributes
(extracted from source data)
Compound status
probe
Member status
virtual
MOA
Signal transduction modulator
Protein Kinase C (PKC) Inhibitors
"Signal transduction modulator
Protein Kinase C (PKC) Inhibitors"
Cellular injury category
Kinase
Target
antibiotic
Apoptosis
Bacterial
Fungal
PKA
PKC
ADC Cytotoxin,Antineoplastic and Immunosuppressive Antibiotics,CaMK,PKA,PKC,PKG,S6 Kinase
Pathway
Anti-infection
Epigenetics
Stem Cell/Wnt
TGF-beta/Smad
Nuisance MOA
Nonspecific kinase inhibition
Targets
Protein kinase C Receptor tyrosine kinases
Source data