General
Preferred name
SU9516
Synonyms
SU 9516 ()
SU-9516 ()
INDIRUBIN SULFATE ()
P&D ID
PD002646
CAS
377090-84-1
666837-93-0
Tags
available
drug candidate
Drug indication
Discovery agent
Drug Status
experimental
investigational
Max Phase
1.0
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 SU9516 is a potent inhibitor of several cyclin-dependent kinases (CDKs) with selectivity for CDK2 .
DESCRIPTION SU9516 is a potent inhibitor of several cyclin-dependent kinases (CDKs) with reported selectivity for CDK2 . Later analysis of SU9516's selectivity profile indicates a similar level of potency as an inhibitor of CDK5/p25 compared to CDK2 . Inhibition of CDK5 was confirmed in a cellular assay measuring dephosphorylation of pFAK(S732). SU9516 also arrests cells at the G2/M phase in cells lacking CDK2, in which case it must be causing the cell cycle arrest via inhibition of CDK1 . (GtoPdb)
DESCRIPTION SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also shows inhibitory effects on CDK1 and CDK4, with IC50s of 40, 200 nM, respectively.
PRICE 65
PRICE 131
DESCRIPTION SU9516 is a selectively potent ATP-competitive inhibitor of CDKs.
DESCRIPTION Selective inhibitor of p38alpha and p38beta2 (Tocris Bioactive Compound Library)
DESCRIPTION Potent cdk2 inhibitor (Tocriscreen Plus)
DESCRIPTION Cylcin-dependent kinase-2 (Cdk-2) inhibitor; induces apoptosis in colon cancer cells (LOPAC library)
DESCRIPTION SU 9516 is a potent, selective cdk2 inhibitor (IC50 values are 0.022, 0.04, >10, >10, 18 and >100 μM for cdk2, cdk1, cdk4, PKC, p38, PDGFR and EGFR respectively). Inhibits pRb phosphorylation causing enhanced pRB/E2F complex formation and induces G1 and G2-M cell cycle arrest. Transcriptionally downregulates Mcl-1 and has antiproliferative, cytostatic and proapoptotic effects in vitro. (BOC Sciences Bioactive Compounds)
DESCRIPTION SU9516 is a potent and selective CDK2 inhibitor, with an IC50 of 17.3 nM. It also inhibits Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1. (Enamine Bioactive Compounds)
DESCRIPTION SU9516 is a potent CDK2 inhibitor with an IC50 of 22 nM and also inhibits CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively. (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
3
Compound Sets
21
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
CDK inhibitor database (CDKiDB)
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
Enamine Bioactive Compounds
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
External IDs
40
Properties
(calculated by RDKit )
Molecular Weight
241.09
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
2
Ring Count
3
Aromatic Ring Count
2
cLogP
1.91
TPSA
67.01
Fraction CSP3
0.08
Chiral centers
0.0
Largest ring
6.0
QED
0.79
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
Enzymes
Selectivity
Cdk2
Primary Target
Cyclin-Dependent Protein Kinases
MOA
Inhibitor
CDK inhibitor
Target
CDK1, CDK2, CDK4, CDK5
CDK
CDK1
CDK2
CDK4
p38
PKC
Pathway
Apoptosis
Autophagy
Cell Cycle/Checkpoint
Chromatin/Epigenetic
Cytoskeletal Signaling
MAPK
Cell Cycle/DNA Damage
Source data