Home DNA Damage/DNA Repair ATM/ATR inhibitor VE-821 For research use only.

VE-821

Synonyms: ATR inhibitor IV

VE-821(ATR inhibitor IV) is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.

VE-821 Chemical Structure

VE-821 Chemical Structure

CAS: 1232410-49-9

Selleck's VE-821 has been cited by 235 publications

Purity & Quality Control

Batch: Purity: 99.74%
99.74

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U2OS  Growth Inhibition Assay IC50～0.8 μM 25593184
SAOS2 Growth Inhibition Assay IC50～0.8 μM 25593184
CAL72 Growth Inhibition Assay IC50～0.8 μM 25593184
NOS1 Growth Inhibition Assay IC50～0.8 μM 25593184
HUO9 Growth Inhibition Assay IC50～0.8 μM 25593184
MG63 Growth Inhibition Assay IC50～9 μM 25593184
SJSA1 Growth Inhibition Assay IC50～9 μM 25593184
MDA-MB-231 Cytotoxicity Assay 1/3/10 μM 1 h potentiates the cytotoxicity of both camptothecin and LMP-400 25269479
HT-29 Cytotoxicity Assay 1/3/10 μM 1 h potentiates the cytotoxicity of both camptothecin and LMP-400 25269479
HCT-116 p53+/+ Cytotoxicity Assay 1/3/10 μM 1 h potentiates the cytotoxicity of both camptothecin and LMP-400 25269479
HCT-116 p53-/- Cytotoxicity Assay 1/3/10 μM 1 h potentiates the cytotoxicity of both camptothecin and LMP-400 25269479
TF-1 Growth Inhibition Assay 0.011–8 μM 96 h enhances the antiproliferative effects of MK1775 24179152
HEL Growth Inhibition Assay 0.011–8 μM 96 h enhances the antiproliferative effects of MK1775 24179152
THP-1 Growth Inhibition Assay 0.011–8 μM 96 h enhances the antiproliferative effects of MK1775 24179152
HL-60  Function Assay 10 mM 0.5 h reduces phosphorylation of Chk1 at serine 345 23934411
OVCAR-8  Function Assay 1 µM  24 h abrogates chemotherapy-induced cell cycle arrest 23548269
PANC-1 Growth Inhibition Assay 0.11-9 μM 1 h inhibits the cell viability in a dose- dependent manner 22825331
MiaPaCa Growth Inhibition Assay 0.11-9 μM 1 h inhibits the cell viability in a dose- dependent manner 22825331
PSN-1 Growth Inhibition Assay 0.11-9 μM 1 h inhibits the cell viability in a dose- dependent manner 22825331
K562 Apoptosis assay 10 uM 48 hrs Induction of apoptosis in human K562 cells assessed as gammaH2AX/53BP1 levels at 10 uM after 48 hrs by DAPI staining based immunofluorescence microscopy in presence of 25 to 250 pM (-)-lomaiviticin A 27177826
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
MDCK Cytotoxicity assay 500 nM 1 hr Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability at 500 nM pretreated for 1 hr followed by 2 Gy irradiation under normoxic condition by Alamar blue assay 27823879
MDCK Cytotoxicity assay 500 nM 1 hr Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability at 500 nM pretreated for 1 hr followed by 4 Gy irradiation under anoxic condition by Alamar blue assay 27823879
MDCK Cytotoxicity assay 500 nM 72 hrs Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability at 500 nM pretreated for 72 hrs followed by 72 hrs incubation under normoxic condition by Alamar blue assay 27823879
MDCK Cytotoxicity assay 500 nM 72 hrs Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability at 500 nM after 72 hrs under anoxic condition by Alamar blue assay 27823879
Click to View More Cell Line Experimental Data

Biological Activity

Description VE-821(ATR inhibitor IV) is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.
Targets
ATR [1]
(Cell-free assay)
13 nM(Ki)
In vitro
In vitro

VE-821(ATR inhibitor IV) shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-PK, mTOR and PI3K (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively. VE-821 alone commits a large fraction of cancer cell populations to death, but it only reversibly limits cell cycle progression in normal cells, with minimal death or long-term detrimental effects. VE-821 along with cisplatin treatment shows the most marked synergy. [1]

VE-821(ATR inhibitor IV) inhibits H2AX cell growth with IC50 of 800 nM. [2]
Kinase Assay Kinase inhibition
The ability of compounds to inhibit ATR, ATM or DNAPK kinase activity istested using a radiometric-phosphate incorporation assay. A stock solution isprepared consisting of the appropriate buffer, kinase, and target peptide. To this isadded the compound of interest, at varying concentrations in DMSO to a final DMSO concentration of 7%. Assays are initiated by addition of an appropriate [γ-33P]ATP solution and incubated at 25 ℃. Assays are stopped, after the desired time course, by addition of phosphoric acid and ATP to a final concentration of 100 mM and 0.66μM, respectively. Peptides are captured on a phosphocellulose membrane, prepared as per manufacturer
Cell Research Cell lines H2AX cells
Concentrations --
Incubation Time 96 hours
Method

Cells are plated in 96-well plates and allowed to adhere overnight. The following day, compounds are added at the indicated concentrations in a final volume of 200μL, and the cells are then incubated for 96 h. MTS reagent (40μL) isthen added, and 1 h later, absorbance at 490 nm ismeasured using a SpectraMax Plus 384 plate reader. Synergy and antagonism are assessed using Macsynergy software.
Experimental Result Images Methods Biomarkers Images PMID
Western blot E-cadherin / Vimentin / ZEB1 Vimentin p-AKT / AKT / p-ERK / ERK 29157079
Growth inhibition assay Cell viability 29157079
In Vivo
In vivo

VE-821(ATR inhibitor IV) is a potent and selective ATP competitive inhibitor of ATR.
Animal Research Animal Models Male immunodefcient mice
Dosages 15 mg/kg
Administration i.p.

Chemical lnformation & Solubility

Molecular Weight 368.41 Formula

C18H16N4O3S
CAS No. 1232410-49-9 SDF Download VE-821 SDF
Smiles CS(=O)(=O)C1=CC=C(C=C1)C2=CN=C(C(=N2)C(=O)NC3=CC=CC=C3)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 74 mg/mL ( (200.86 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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