For research use only.

Catalog No.S8007

118 publications

VE-821 Chemical Structure

Molecular Weight(MW): 368.41

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 118 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.
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  NUWxZXI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PDUWlEPTExv[6wMlgh|ryP MWeyOVU6OzF6NB?=
SAOS2 NXzmNXZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGixbmpKSzVy784eNE45KM7:TR?= NIP2Z|YzPTV7M{G4OC=>
CAL72 NUD4U|RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TnOmlEPTExv[6wMlgh|ryP MoDxNlU2QTNzOES=
NOS1 M1rIbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vVcGlEPTExv[6wMlgh|ryP NX7JRYNiOjV3OUOxPFQ>
HUO9 NX\rXXZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nnTmlEPTExv[6wMlgh|ryP NEjNfVczPTV7M{G4OC=>
MG63 NHPpZndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDWTWM2OO,;nkmg{txO NVPFOGh1OjV3OUOxPFQ>
SJSA1 MlywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|Ux973gOTFOwG0> MUmyOVU6OzF6NB?=
MDA-MB-231 MknER5l1d3SxeHnjbZR6KEG|c3H5 M{\yPFEwOy9zMDFOwG0> NUHp[XYyOSCq NIPmXHFxd3SnboTpZZRmeyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHLveIgh[2GvcITveIhm[2mwIHHu[EBNVVBvNECw NXjxdGY3OjV{Nkm0O|k>
HT-29 M1XC[2N6fG:2b4jpZ4l1gSCDc4PhfS=> M3rNbVEwOy9zMDFOwG0> Mn;KNUBp M2PxcpBwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiYn;0bEBk[W2ydH;0bIVkcW5iYX7kJGxOWC12MEC= MljkNlUzPjl2N{m=
HCT-116 p53+/+ NEDTcVNEgXSxdH;4bYNqfHliQYPzZZk> NUfpS3FnOS9|L{GwJO69VQ>? MVuxJIg> NFWwcmFxd3SnboTpZZRmeyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHLveIgh[2GvcITveIhm[2mwIHHu[EBNVVBvNECw MWKyOVI3QTR5OR?=
HCT-116 p53-/- M2LuN2N6fG:2b4jpZ4l1gSCDc4PhfS=> M4LXeVEwOy9zMDFOwG0> NYi5dppQOSCq NH3KSFNxd3SnboTpZZRmeyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHLveIgh[2GvcITveIhm[2mwIHHu[EBNVVBvNECw M{\GZVI2OjZ7NEe5
TF-1 M2TzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\5dFAvODFz4pETPEDPxE1? NY\leGkyQTZiaB?= NGXTTlJmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1eyCxZjDNT|E4PzV? MViyOFE4QTF3Mh?=
HEL NUP5TGl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;sNE4xOTIkgKO4JO69VQ>? NFPtU2c6PiCq NYrOdVlk\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfHNib3[gUWsyPzd3 NFO3S5kzPDF5OUG1Ni=>
THP-1 MknoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3jOoFWOC5yMUJihLM5KM7:TR?= NWPaTVdwQTZiaB?= NHvXTm9mdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1eyCxZjDNT|E4PzV? NYjiZY9yOjRzN{mxOVI>
HL-60  NHr3d3RHfW6ldHnvckBCe3OjeR?= MkP0NVAhdU1? MoHvNE42KGh? M{T6TpJm\HWlZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGNpczFiYYSgd4VzcW6nIEO0OS=> MVqyN|k{PDRzMR?=
OVCAR-8  MYfGeY5kfGmxbjDBd5NigQ>? M2f6OVEhyrWPwrC= NGPYXm4zPCCq NUDidXhZ[WK{b3fheIV{KGOqZX3veIhmemGyeT3pcoR2[2WmIHPlcIwh[3mlbHWgZZJz\XO2 Mn3JNlM2PDh{Nkm=
PANC-1 NXvZc4hwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXDUWs1OC5zMT25JO69VQ>? NY[0flVUOSCq NYDuNZVJcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? MUiyNlgzPTN|MR?=
MiaPaCa MorpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXCNE4yOS17IN88US=> NEPDdFYyKGh? MVfpcohq[mm2czD0bIUh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMUBl\XCnbnTlcpQhdWGwbnXy M2jielIzQDJ3M{Ox
PSN-1 NI\HW4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWW1OW5pOC5zMT25JO69VQ>? MVqxJIg> MoDwbY5pcWKrdIOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U0h\GWyZX7k[Y51KG2jbn7ldi=> MWCyNlgzPTN|MR?=

... Click to View More Cell Line Experimental Data

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.


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.

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.



Kinase Assay:


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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:


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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


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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID