Catalog No.S8007

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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4 Customer Reviews

  • Cell viability response to ATR inhibitor.

    Nature, 2018, 555(7696):387-391. VE-821 purchased from Selleck.

    (C) VCaP cells were treated with T-474 together with the ATR inhibitor VE-821, ATM inhibitor KU-55933, or DNA-PK inhibitor NU7026 as indicated for 4 days. Cell viability was measured (N = 3, mean with SD). *P < 0.01 and **P < 0.000001; N.S., not significant (P > 0.05).

    Oncotarget, 2018, 9(17): 13474-13487. VE-821 purchased from Selleck.

  • Western blot for γH2AX in H460 cells treated with Cr(VI) in the presence of a second set of inhibitors (ATM-i2—10 uM KU55933, DNAPK-i2—10 uM NU7441, ATR-i2—10 uM VE821). “γH2AX-total” numbers indicate a total normalized intensity of both γH2AX bands from 2 Western blots.

    Toxicol Sci 2014 10.1093/toxsci/kfu207. VE-821 purchased from Selleck.

    Western blot analysis of phospho-p53 and total p53 in H1 cells treated with 2 uM MNNG and the ATM-specific inhibitor KU5593, the ATR-specific inhibitor VE-821, or both for 24 h. The values represent the means of three independent experiments. Error bars represent S.E.

    J Biol Chem 2014 289(35), 24314-24. VE-821 purchased from Selleck.

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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  MkPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;HdmZnUUN3MP-9olAvQCEQvF2= M13IeVI2PTl|MUi0
SAOS2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7QW4hUUUN3MP-9olAvQCEQvF2= NH6zT5gzPTV7M{G4OC=>
CAL72 M4D6VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITzcFZKSzVy784eNE45KM7:TR?= M{K4VlI2PTl|MUi0
NOS1 M4DQZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|Ux973gMD64JO69VQ>? M4ew[lI2PTl|MUi0
HUO9 NIC0d4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3YW|lEUUN3MP-9olAvQCEQvF2= Mlq4NlU2QTNzOES=
MG63 NEHDZVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPuTWM2OO,;nkmg{txO MWeyOVU6OzF6NB?=
SJSA1 NEL6bYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWWyNZNnUUN3MP-9olkh|ryP NGrKVmEzPTV7M{G4OC=>
MDA-MB-231 NEf1XJNEgXSxdH;4bYNqfHliQYPzZZk> M2Ptd|EwOy9zMDFOwG0> M2jTc|EhcA>? MX;wc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy NEXNWoYzPTJ4OUS3PS=>
HT-29 NFXGUlJEgXSxdH;4bYNqfHliQYPzZZk> M1TJSlEwOy9zMDFOwG0> NHvpRmMyKGh? NFfpU45xd3SnboTpZZRmeyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHLveIgh[2GvcITveIhm[2mwIHHu[EBNVVBvNECw NGjSRlUzPTJ4OUS3PS=>
HCT-116 p53+/+ NYHIO2FxS3m2b4TvfIlkcXS7IFHzd4F6 M{fyOVEwOy9zMDFOwG0> MXWxJIg> NHj2SXFxd3SnboTpZZRmeyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHLveIgh[2GvcITveIhm[2mwIHHu[EBNVVBvNECw MnWwNlUzPjl2N{m=
HCT-116 p53-/- MVzDfZRwfG:6aXPpeJkhSXO|YYm= NV;zW5BpOS9|L{GwJO69VQ>? MWKxJIg> NHv6[mNxd3SnboTpZZRmeyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHLveIgh[2GvcITveIhm[2mwIHHu[EBNVVBvNECw M3G1OVI2OjZ7NEe5
TF-1 M2HVWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmwMlAyOeLCk{ig{txO NXPscFRqQTZiaB?= NYC3Vot5\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfHNib3[gUWsyPzd3 Ml72NlQyPzlzNUK=
HEL M4TWXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofRNE4xOTIkgKO4JO69VQ>? NGjhb5Q6PiCq M4[1TIVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5R{KG:oIF3LNVc4PQ>? NE[yVoszPDF5OUG1Ni=>
THP-1 M{Sxbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonTNE4xOTIkgKO4JO69VQ>? MVy5OkBp MmTp[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMhd2ZiTVuxO|c2 MmfONlQyPzlzNUK=
HL-60  MX3GeY5kfGmxbjDBd5NigQ>? M13sW|ExKG2P NUHkdYE2OC53IHi= MoT0doVlfWOnczDwbI9{eGixconsZZRqd25ib3[gR4hsOSCjdDDz[ZJqdmViM{S1 MYGyN|k{PDRzMR?=
OVCAR-8  M1vjW2Z2dmO2aX;uJGF{e2G7 MU[xJOK2VcLi M2jmPFI1KGh? NF7nVGNi[nKxZ3H0[ZMh[2inbX;0bIVz[XC7LXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3R? Mn\WNlM2PDh{Nkm=
PANC-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XGblAvOTFvOTFOwG0> Ml7CNUBp NVjlUnp6cW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? NETvUIIzOjh{NUOzNS=>
MiaPaCa MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXiwMlEyNTlizszN NXrkSXcxOSCq MULpcohq[mm2czD0bIUh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMUBl\XCnbnTlcpQhdWGwbnXy M{n2dFIzQDJ3M{Ox
PSN-1 NVL1Nm1OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7tUHIxNjFzLUmg{txO Mo\FNUBp Mo\obY5pcWKrdIOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U0h\GWyZX7k[Y51KG2jbn7ldi=> NH3KUW8zOjh{NUOzNS=>

... Click to View More Cell Line Experimental Data


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

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID