VE-821

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.

Size Price Stock Quantity  
USD 147 In stock
USD 470 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

2 Customer Reviews

  • 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.

    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.

Purity & Quality Control

Choose Selective ATM/ATR Inhibitors

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  MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrXTWM2OO,;nkCuPEDPxE1? NIrw[2IzPTV7M{G4OC=>
SAOS2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|Ux973gMD64JO69VQ>? MnLoNlU2QTNzOES=
CAL72 NEnocVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jE[WlEPTExv[6wMlgh|ryP MW[yOVU6OzF6NB?=
NOS1 MknxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHmTWM2OO,;nkCuPEDPxE1? MUCyOVU6OzF6NB?=
HUO9 NH31SGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIq2cYVKSzVy784eNE45KM7:TR?= MlTSNlU2QTNzOES=
MG63 NWXCVopxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|Ux973gOTFOwG0> MXiyOVU6OzF6NB?=
SJSA1 MnK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLqZo1KSzVy784ePUDPxE1? NV\PWWhLOjV3OUOxPFQ>
MDA-MB-231 Mlj5R5l1d3SxeHnjbZR6KEG|c3H5 M4TJVFEwOy9zMDFOwG0> M4nrfVEhcA>? NVraN4RxeG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> NY\me21uOjV{Nkm0O|k>
HT-29 NWDFTFNbS3m2b4TvfIlkcXS7IFHzd4F6 M3;nPFEwOy9zMDFOwG0> M{nrTVEhcA>? MXHwc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy M4jlVlI2OjZ7NEe5
HCT-116 p53+/+ Mmf0R5l1d3SxeHnjbZR6KEG|c3H5 MVixM|MwOTBizszN M4PpV|EhcA>? Mn3sdI91\W62aXH0[ZMhfGinIHP5eI91d3irY3n0fUBw\iCkb4ToJINidXC2b4To[YNqdiCjbnSgUG1RNTRyMB?= MmHKNlUzPjl2N{m=
HCT-116 p53-/- NIO2fnBEgXSxdH;4bYNqfHliQYPzZZk> NE\4VXAyNzNxMUCg{txO MU[xJIg> MkW2dI91\W62aXH0[ZMhfGinIHP5eI91d3irY3n0fUBw\iCkb4ToJINidXC2b4To[YNqdiCjbnSgUG1RNTRyMB?= NEnDTmUzPTJ4OUS3PS=>
TF-1 NGfrVodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\FZlAvODFz4pETPEDPxE1? NU\DN3o{QTZiaB?= NHXMXGRmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1eyCxZjDNT|E4PzV? MUmyOFE4QTF3Mh?=
HEL M{nOdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjSNE4xOTIkgKO4JO69VQ>? NYDpSodMQTZiaB?= Mmrw[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMhd2ZiTVuxO|c2 NH\ySpYzPDF5OUG1Ni=>
THP-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7ENE4xOTIkgKO4JO69VQ>? NUXEVZdQQTZiaB?= Mmnx[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMhd2ZiTVuxO|c2 Mlz2NlQyPzlzNUK=
HL-60  NVWyW3llTnWwY4Tpc44hSXO|YYm= MV[xNEBuVQ>? NYLCPGRQOC53IHi= NGrCfWRz\WS3Y3XzJJBpd3OyaH;yfYxifGmxbjDv[kBEcGtzIHH0JJNmemmwZTCzOFU> NHv1bIszOzl|NESxNS=>
OVCAR-8  NFPQZWNHfW6ldHnvckBCe3OjeR?= NWrjbm9sOSEEtV5CpC=> MonsNlQhcA>? MUHhZpJw\2G2ZYOgZ4hmdW:2aHXyZZB6NWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5Q> NU\xcoRIOjN3NEiyOlk>
PANC-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LxRVAvOTFvOTFOwG0> MWmxJIg> MWnpcohq[mm2czD0bIUh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMUBl\XCnbnTlcpQhdWGwbnXy NFvt[2kzOjh{NUOzNS=>
MiaPaCa MljlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:xdHExNjFzLUmg{txO MmP5NUBp MUXpcohq[mm2czD0bIUh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMUBl\XCnbnTlcpQhdWGwbnXy NGjNfpIzOjh{NUOzNS=>
PSN-1 NIm3UpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlq5NE4yOS17IN88US=> MVOxJIg> M4f5[IlvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4UuKGSncHXu[IVvfCCvYX7u[ZI> NXPTXpl[OjJ6MkWzN|E>

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:

[2]

+ Expand

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]

+ Expand
  • 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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

ATM/ATR Signaling Pathway Map

ATM/ATR Inhibitors with Unique Features

Related ATM/ATR Products

Tags: buy VE-821 | VE-821 supplier | purchase VE-821 | VE-821 cost | VE-821 manufacturer | order VE-821 | VE-821 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID