VE-821

For research use only.

Catalog No.S8007

139 publications

VE-821 Chemical Structure

CAS No. 1232410-49-9

VE-821 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.

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10mM (1mL in DMSO) USD 191 In stock
USD 147 In stock
USD 470 In stock
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Selleck's VE-821 has been cited by 139 publications

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Biological Activity

Description VE-821 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

VE-821 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 inhibits H2AX cell growth with IC50 of 800 nM. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U2OS  MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzZcIRKUUN3MP-9olAvQCEQvF2= Moj1NlU2QTNzOES=
SAOS2 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVL0T41FUUN3MP-9olAvQCEQvF2= NXz5dVl[OjV3OUOxPFQ>
CAL72 MoPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jWT2lEPTExv[6wMlgh|ryP M1\ncFI2PTl|MUi0
NOS1 Mk\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX75eWdXUUN3MP-9olAvQCEQvF2= MXWyOVU6OzF6NB?=
HUO9 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vB[mlEPTExv[6wMlgh|ryP M2DPWFI2PTl|MUi0
MG63 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\IWXhzUUN3MP-9olkh|ryP NUnPXoYyOjV3OUOxPFQ>
SJSA1 NUD3bG5bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|Ux973gOTFOwG0> MXmyOVU6OzF6NB?=
MDA-MB-231 NV3Yd2tVS3m2b4TvfIlkcXS7IFHzd4F6 NVTJXZJSOS9|L{GwJO69VQ>? NYXNO3lzOSCq MUPwc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy NH75NG0zPTJ4OUS3PS=>
HT-29 MnLBR5l1d3SxeHnjbZR6KEG|c3H5 MknYNU8{NzFyIN88US=> M3zROFEhcA>? M4Xze5BwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiYn;0bEBk[W2ydH;0bIVkcW5iYX7kJGxOWC12MEC= MoraNlUzPjl2N{m=
HCT-116 p53+/+ NXPPV4s4S3m2b4TvfIlkcXS7IFHzd4F6 MYOxM|MwOTBizszN NVHNdm1yOSCq MXLwc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy MXyyOVI3QTR5OR?=
HCT-116 p53-/- MVrDfZRwfG:6aXPpeJkhSXO|YYm= MnfFNU8{NzFyIN88US=> NV;mfGtXOSCq MXvwc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy NHezNmUzPTJ4OUS3PS=>
TF-1 MnHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\QVVAvODFz4pETPEDPxE1? NETVU5I6PiCq M2PLUIVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5R{KG:oIF3LNVc4PQ>? M3LGblI1OTd7MUWy
HEL M2XW[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH2w[oExNjBzMfMAl|gh|ryP NH3FOIM6PiCq NYXoNI1n\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfHNib3[gUWsyPzd3 M3u2cVI1OTd7MUWy
THP-1 MlHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmwMlAyOeLCk{ig{txO Mm\FPVYhcA>? Mlvj[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMhd2ZiTVuxO|c2 NFHuTpozPDF5OUG1Ni=>
HL-60  NVPKSHFpTnWwY4Tpc44hSXO|YYm= NF6yPVgyOCCvTR?= M4f1W|AvPSCq MmrYdoVlfWOnczDwbI9{eGixconsZZRqd25ib3[gR4hsOSCjdDDz[ZJqdmViM{S1 NHrnPJgzOzl|NESxNS=>
OVCAR-8  M2DDUWZ2dmO2aX;uJGF{e2G7 M2LRXlEhyrWPwrC= NUSxcmNGOjRiaB?= MorWZYJzd2ejdHXzJINp\W2xdHjldoFxgS2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1 M3O4SFI{PTR6Mk[5
PANC-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGwMlEyNTlizszN M2DPfVEhcA>? NVLGfGp7cW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? NFy0bG4zOjh{NUOzNS=>
MiaPaCa MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\uNE4yOS17IN88US=> M3jNdFEhcA>? NIrHSpNqdmirYnn0d{B1cGViY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNSCmZYDlcoRmdnRibXHucoVz M4LVXVIzQDJ3M{Ox
PSN-1 M1vnZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3e3NlAvOTFvOTFOwG0> MWGxJIg> NUHLR5pqcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? NFXiR5AzOjh{NUOzNS=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
E-cadherin / Vimentin / ZEB1 ; 

PubMed: 29157079     


Four kinds of cancer cells were treated with 5 μM VE-821 for 24 h and 48 h. The expression of E-cadherin, Vimentin and ZEB1 was performed by Western Blotting. Actin was used as loading control.

Vimentin; 

PubMed: 29157079     


(D) MGC-803 cells were stained with antibodies to Vimentin (green) and nuclei was stained with DAPI. Images were captured by fluorescence microscopy at × 40 magnification.

p-AKT / AKT / p-ERK / ERK ; 

PubMed: 29157079     


HCT-116 and NCI-N87 cells were added to 5 μM VE-821 for 24 h and 48 h. The total and phosphorylation expression of AKT and ERK was performed by Western Blotting.

29157079
Growth inhibition assay
Cell viability; 

PubMed: 29157079     


Indicated concentrations of VE-821 (0, 1, 5 and 10 μM) were added to four kinds of cancer cells (PANC-1, MGC-803, HCT-116 and NCI-N87) for 48 h. Cell viability was performed by MTT assay. Results from three independent experiments are shown.

29157079

Protocol

Kinase Assay:

[2]

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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:

[2]

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  • 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (200.86 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 368.41
Formula

C18H16N4O3S

CAS No. 1232410-49-9
Storage powder
in solvent
Synonyms N/A
Smiles CS(=O)(=O)C1=CC=C(C=C1)C2=CN=C(C(=N2)C(=O)NC3=CC=CC=C3)N

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID