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  
In DMSO USD 191 In stock
USD 147 In stock
USD 470 In stock

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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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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  MoOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|Ux973gMD64JO69VQ>? NWnjbIRZOjV3OUOxPFQ>
SAOS2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnKxTWM2OO,;nkCuPEDPxE1? NYfmOWhMOjV3OUOxPFQ>
CAL72 MmHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DCOWlEPTExv[6wMlgh|ryP NUftSpp4OjV3OUOxPFQ>
NOS1 NH\6R2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HhSmlEPTExv[6wMlgh|ryP M2\wXlI2PTl|MUi0
HUO9 MmXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrUWGRKSzVy784eNE45KM7:TR?= M135[|I2PTl|MUi0
MG63 NEjVbpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|Ux973gOTFOwG0> M2HzUlI2PTl|MUi0
SJSA1 M3r4emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmGzTWM2OO,;nkmg{txO NUe1XlhqOjV3OUOxPFQ>
MDA-MB-231 NWDXeI82S3m2b4TvfIlkcXS7IFHzd4F6 M4LiZVEwOy9zMDFOwG0> MVSxJIg> NYK3RVdWeG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> NFnYNoEzPTJ4OUS3PS=>
HT-29 NYnreFd1S3m2b4TvfIlkcXS7IFHzd4F6 MVKxM|MwOTBizszN NVLHdm1zOSCq NWTHTFBDeG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> MnXzNlUzPjl2N{m=
HCT-116 p53+/+ NHr0eY9EgXSxdH;4bYNqfHliQYPzZZk> NUjUZYh[OS9|L{GwJO69VQ>? M3vybFEhcA>? MWjwc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy NVj6TWdJOjV{Nkm0O|k>
HCT-116 p53-/- M2HRUGN6fG:2b4jpZ4l1gSCDc4PhfS=> NYrvVWNwOS9|L{GwJO69VQ>? NYPxXGtLOSCq MYLwc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy NFnJWYIzPTJ4OUS3PS=>
TF-1 M1jMTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVuwMlAyOeLCk{ig{txO NFz2VVk6PiCq M1qwTYVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5R{KG:oIF3LNVc4PQ>? MVKyOFE4QTF3Mh?=
HEL MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnBc3NKOC5yMUJihLM5KM7:TR?= NUHqOZpNQTZiaB?= MUflcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0d{Bw\iCPS{G3O|U> Mn3SNlQyPzlzNUK=
THP-1 Ml;6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zvd|AvODFz4pETPEDPxE1? MWi5OkBp Mlnh[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMhd2ZiTVuxO|c2 M3vmOVI1OTd7MUWy
HL-60  M3O5[mZ2dmO2aX;uJGF{e2G7 M17KWVExKG2P NXTXVYc3OC53IHi= MWfy[YR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDDbIsyKGG2IIPldolv\SB|NEW= NHjj[4wzOzl|NESxNS=>
OVCAR-8  MX7GeY5kfGmxbjDBd5NigQ>? NGjxWJUyKML3TdMg M17uN|I1KGh? NX\kPYxW[WK{b3fheIV{KGOqZX3veIhmemGyeT3pcoR2[2WmIHPlcIwh[3mlbHWgZZJz\XO2 NF;2R5IzOzV2OEK2PS=>
PANC-1 NUjEeGlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\GWGtnOC5zMT25JO69VQ>? NXfvPIx6OSCq NHXkNpFqdmirYnn0d{B1cGViY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNSCmZYDlcoRmdnRibXHucoVz NFLvU4szOjh{NUOzNS=>
MiaPaCa MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[4NE4yOS17IN88US=> NYC2dIFrOSCq M3jCXIlvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4UuKGSncHXu[IVvfCCvYX7u[ZI> M{m5dVIzQDJ3M{Ox
PSN-1 NXTBcJg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqwMlEyNTlizszN MlryNUBp M4HkeolvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4UuKGSncHXu[IVvfCCvYX7u[ZI> MV:yNlgzPTN|MR?=

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay
+ 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's instructions, and washed six times with 200 μL of 100 mM phosphoric acid, prior to the addition of 100 μL of scintillation cocktail and scintillation counting on a 1450 Microbeta Liquid Scintillation Counter. Dose−response data are analyzed using GraphPad Prism software

Solubility (25°C)

In vitro DMSO 74 mg/mL (200.86 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

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)

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*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 )

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* 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

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  • Computed Result

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Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID