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.

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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

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  M33GTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXQTWM2OO,;nkCuPEDPxE1? NWDDZ2RKOjV3OUOxPFQ>
SAOS2 NFfxd2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjT[|hKSzVy784eNE45KM7:TR?= M3PndFI2PTl|MUi0
CAL72 NYDYO45kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|Ux973gMD64JO69VQ>? MWWyOVU6OzF6NB?=
NOS1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13QdmlEPTExv[6wMlgh|ryP MlLUNlU2QTNzOES=
HUO9 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjnbJVKSzVy784eNE45KM7:TR?= MkHSNlU2QTNzOES=
MG63 NUjYUlZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnFTWM2OO,;nkmg{txO MomwNlU2QTNzOES=
SJSA1 NXTCcW5GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|Ux973gOTFOwG0> MoTQNlU2QTNzOES=
MDA-MB-231 MVjDfZRwfG:6aXPpeJkhSXO|YYm= MoTWNU8{NzFyIN88US=> M1\Td|EhcA>? MWrwc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy MX[yOVI3QTR5OR?=
HT-29 NGW5dIJEgXSxdH;4bYNqfHliQYPzZZk> NGr3PZYyNzNxMUCg{txO MXqxJIg> M4KxO5BwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiYn;0bEBk[W2ydH;0bIVkcW5iYX7kJGxOWC12MEC= M1nzcVI2OjZ7NEe5
HCT-116 p53+/+ MUfDfZRwfG:6aXPpeJkhSXO|YYm= NWfMZYlFOS9|L{GwJO69VQ>? NFj5WIwyKGh? M{Pm[ZBwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiYn;0bEBk[W2ydH;0bIVkcW5iYX7kJGxOWC12MEC= M4rWeVI2OjZ7NEe5
HCT-116 p53-/- MlrsR5l1d3SxeHnjbZR6KEG|c3H5 MoDQNU8{NzFyIN88US=> MXexJIg> NEfIO3Rxd3SnboTpZZRmeyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHLveIgh[2GvcITveIhm[2mwIHHu[EBNVVBvNECw NHLvVowzPTJ4OUS3PS=>
TF-1 NY[3WlNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[5enAyOC5yMUJihLM5KM7:TR?= NIPRZmI6PiCq Mlnu[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMhd2ZiTVuxO|c2 MYmyOFE4QTF3Mh?=
HEL NXjCUlhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PCbVAvODFz4pETPEDPxE1? NVLVXHFEQTZiaB?= NGW1WmhmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1eyCxZjDNT|E4PzV? M3LkWlI1OTd7MUWy
THP-1 NUWyPXJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTINE4xOTIkgKO4JO69VQ>? NFLsb3U6PiCq MWDlcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0d{Bw\iCPS{G3O|U> Ml7hNlQyPzlzNUK=
HL-60  NELG[GdHfW6ldHnvckBCe3OjeR?= MX6xNEBuVQ>? MojwNE42KGh? MXLy[YR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDDbIsyKGG2IIPldolv\SB|NEW= NVLCNVVGOjN7M{S0NVE>
OVCAR-8  Ml:1SpVv[3Srb36gRZN{[Xl? NHy0OngyKML3TdMg NYfudVZ{OjRiaB?= NYnvZ|RW[WK{b3fheIV{KGOqZX3veIhmemGyeT3pcoR2[2WmIHPlcIwh[3mlbHWgZZJz\XO2 NFm1boUzOzV2OEK2PS=>
PANC-1 NEHDbXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWewMlEyNTlizszN NUWzb25DOSCq NGi2UZVqdmirYnn0d{B1cGViY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNSCmZYDlcoRmdnRibXHucoVz NHTr[VUzOjh{NUOzNS=>
MiaPaCa MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\1NE4yOS17IN88US=> NX3peJlVOSCq MnrTbY5pcWKrdIOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U0h\GWyZX7k[Y51KG2jbn7ldi=> MX:yNlgzPTN|MR?=
PSN-1 NYfMV4ZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSwMlEyNTlizszN MUmxJIg> MVfpcohq[mm2czD0bIUh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMUBl\XCnbnTlcpQhdWGwbnXy MlHpNlI5OjV|M{G=

... 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'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 slightly soluble or insoluble
Ethanol slightly soluble or 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
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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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