General
Preferred name
PKR-IN-C16
Synonyms
C16 ()
PKR inhibitor ()
ASN-11124542 ()
imoxin, C16, Imidazolo-oxindole PKR inhibitor C16 ()
P&D ID
PD015705
CAS
608512-97-6
Tags
available
drug candidate
Drug indication
Discovery agent
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 PKR-IN-C16 (Compound C16) is a specific double-stranded RNA-dependent protein kinase (PKR) inhibitor. PKR-IN-C16 shows promising neuroprotective properties and can rescue acute brain lesions[1].
PRICE 84
DESCRIPTION This is compound 16 in which has been shown to be an ATP competitive inhibitor blocking autophosphorylation of PKR.
Double-stranded RNA-activated protein kinase (PKR) is also known as eukaryotic initiation factor 2 subunit α (eIF2α). (GtoPdb)
DESCRIPTION C16 is an inhibitor of RNA-activated protein kinase (PKR) (IC50 = 210 nM). It is an imidazolo-oxindole derivative that binds to ATP-binding site of PKR and rescues PKR-dependent translation block in vitro. C16 has neuroprotective activity against cell damage in human neuroblastoma cells and neuroinflammation in acute excitotoxic rat model. (BOC Sciences Bioactive Compounds)
DESCRIPTION PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.PKR-IN-C16 binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM. PKR-IN-C16 protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress. (TargetMol Bioactive Compound Library)
DESCRIPTION Potent RET inhibitor (Tocris Bioactive Compound Library)
Compound Sets
12
AdooQ Bioactive Compound Library
A13538
BOC Sciences Bioactive Compounds
c16-cas-608512-97-6-376217
Cayman Chemical Bioactives
15323
CZ-OPENSCREEN Bioactive Library
DrugMAP
DMFNZOI
Guide to Pharmacology
6026
Mcule NIBR MoA Box Subset
MCULE-5829692005
MedChem Express Bioactive Compound Library
HY-13977A
Novartis Chemogenetic Library (NIBR MoA Box)
Selleckchem Bioactive Compound Library
pkr-in-c16
TargetMol Bioactive Compound Library
T16550
Tocris Bioactive Compound Library
5382
External IDs
18
Properties
(calculated by RDKit )
Molecular Weight
268.04
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
2
Rotatable Bonds
1
Ring Count
4
Aromatic Ring Count
3
cLogP
2.51
TPSA
70.67
Fraction CSP3
0.0
Chiral centers
0.0
Largest ring
6.0
QED
0.67
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
PKR
Apoptosis
Apoptosis related,eIF,Interleukins,PKR
Primary Target
Other Kinases
MOA
Inhibitor
PKR Inhibitor
Member status
member
Source data