General
Preferred name
NU7441
Synonyms
NU-7441 ()
KU-57788 ()
KU 57788 ()
NU 7441 ()
NU-7441 (KU-57788) ()
NU-7432 ()
NU7441 (KU-57788) ()
P&D ID
PD010903
CAS
503468-95-9
Tags
available
drug candidate
Drug indication
Discovery agent
Probe control
Probe control not defined
Orthogonal probes
0
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)
DESCRIPTION
NU-7441 is a potent and selective, ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK) . It is compound 22g in Leahy et al. (2004) .
(GtoPdb)
DESCRIPTION
KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC50 of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC50s of 5.0 and 1.7 ¦ÌM, respectively[1].
PRICE
77
DESCRIPTION
Stimulates RhoA activation; antiproliferative agent that slows cell cycle progression
(Tocris Bioactive Compound Library)
DESCRIPTION
NU7441 is a highly potent and selective DNA-PK inhibitor (IC50=14 nM), exhibiting ATP-competitive inhibition kinetics. NU7441 increased the cytotoxicity of ionizing radiation and etoposide in SW620, LoVo, and V3-YAC cells but not in V3 cells, confirming that potentiation was due to DNA-PK inhibition. NU7441 substantially retarded the repair of ionizing radiation-induced and etoposide-induced DSB. NU7441 appreciably increased G(2)-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells. In mice bearing SW620 xenografts, NU7441 concentrations in the tumor necessary for chemopotentiation in vitro were maintained for at least 4 hours at nontoxic doses. NU7441 increased etoposide-induced tumor growth delay 2-fold without exacerbating etoposide toxicity to unacceptable levels. In conclusion, NU7441 shows sufficient proof of principle through in vitro and in vivo chemosensitization and radiosensitization to justify further development of DNA-PK inhibitors for clinical use.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
NU7441 (KU-57788 (NU7441)) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM).
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
437
Organisms
1
Compound Sets
18
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
LINCS compound set
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Welcome Trust Cancer Drugs
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
23
Molecular Weight
413.11
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
0
Rotatable Bonds
2
Ring Count
6
Aromatic Ring Count
5
cLogP
5.66
TPSA
42.68
Fraction CSP3
0.16
Chiral centers
0.0
Largest ring
6.0
QED
0.37
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
Genome integrity
Cell Cycle/DNA Damage
PI3K/Akt/mTOR
DNA Damage/DNA Repair
PI3K/Akt/mTOR signaling
Target
DNAPK
CRISPR/Cas9
DNA-PK
PRKDC
DNA-PK inhibitor
CRISPR/Cas9,DNA-PK,mTOR,PI3K
Primary Target
DNA-Dependent Protein Kinase
MOA
Inhibitor
Inhibitors of Signal Transduction Pathways
DNA-Dependent Protein Kinase (DNA-PK) Inhibitors
DNA Repair Inhibitors
"Inhibitors of Signal Transduction Pathways
DNA Repair Inhibitors"
DNA dependent protein kinase inhibitor
Member status
member
Recommended Cell Concentration
None
Source data
