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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3 Customer Reviews

  • (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 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  MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13aOmlEPTExv[6wMlgh|ryP MmrhNlU2QTNzOES=
SAOS2 NVrnSmQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2WwO2lEPTExv[6wMlgh|ryP NEWyOmgzPTV7M{G4OC=>
CAL72 NXH1Z2lJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzTW5FTUUN3MP-9olAvQCEQvF2= MVyyOVU6OzF6NB?=
NOS1 M{PVXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|Ux973gMD64JO69VQ>? NEfRdGQzPTV7M{G4OC=>
HUO9 Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1G0e2lEPTExv[6wMlgh|ryP M4nEflI2PTl|MUi0
MG63 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|Ux973gOTFOwG0> MkfZNlU2QTNzOES=
SJSA1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jsWGlEPTExv[65JO69VQ>? MnnSNlU2QTNzOES=
MDA-MB-231 MVPDfZRwfG:6aXPpeJkhSXO|YYm= NVHIOo02OS9|L{GwJO69VQ>? MYCxJIg> M3XLe5BwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiYn;0bEBk[W2ydH;0bIVkcW5iYX7kJGxOWC12MEC= NXPObYlOOjV{Nkm0O|k>
HT-29 MWfDfZRwfG:6aXPpeJkhSXO|YYm= MVKxM|MwOTBizszN NGfkW2QyKGh? NH3S[XJxd3SnboTpZZRmeyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHLveIgh[2GvcITveIhm[2mwIHHu[EBNVVBvNECw NIGxd5gzPTJ4OUS3PS=>
HCT-116 p53+/+ MVrDfZRwfG:6aXPpeJkhSXO|YYm= NWPpRY5IOS9|L{GwJO69VQ>? NVixOY9ZOSCq NGDNWXNxd3SnboTpZZRmeyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHLveIgh[2GvcITveIhm[2mwIHHu[EBNVVBvNECw M4PvSlI2OjZ7NEe5
HCT-116 p53-/- M1\Hc2N6fG:2b4jpZ4l1gSCDc4PhfS=> MlP5NU8{NzFyIN88US=> NWXhbGZpOSCq M4rUcJBwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiYn;0bEBk[W2ydH;0bIVkcW5iYX7kJGxOWC12MEC= NI\aS5ozPTJ4OUS3PS=>
TF-1 M4rkdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfHWmtYOC5yMUJihLM5KM7:TR?= MYq5OkBp NHnjUYFmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1eyCxZjDNT|E4PzV? M{jEbFI1OTd7MUWy
HEL NF;Vb3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LVNlAvODFz4pETPEDPxE1? M3PZelk3KGh? MUDlcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0d{Bw\iCPS{G3O|U> M13MVFI1OTd7MUWy
THP-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPlPXRQOC5yMUJihLM5KM7:TR?= NHr3eZQ6PiCq M37We4VvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5R{KG:oIF3LNVc4PQ>? NYfuT|l[OjRzN{mxOVI>
HL-60  M{XuRmZ2dmO2aX;uJGF{e2G7 M1ruXVExKG2P M4DiWlAvPSCq Mk\rdoVlfWOnczDwbI9{eGixconsZZRqd25ib3[gR4hsOSCjdDDz[ZJqdmViM{S1 M2Du[VI{QTN2NEGx
OVCAR-8  M4raVWZ2dmO2aX;uJGF{e2G7 NUDBVWp7OSEEtV5CpC=> MWGyOEBp NXzuT4R[[WK{b3fheIV{KGOqZX3veIhmemGyeT3pcoR2[2WmIHPlcIwh[3mlbHWgZZJz\XO2 NUXWbIxXOjN3NEiyOlk>
PANC-1 MoPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjhNIIxNjFzLUmg{txO NIjpTIgyKGh? M3L1bYlvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4UuKGSncHXu[IVvfCCvYX7u[ZI> NHjVeFgzOjh{NUOzNS=>
MiaPaCa MnnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LPUFAvOTFvOTFOwG0> NGHEWGIyKGh? M2XZeIlvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4UuKGSncHXu[IVvfCCvYX7u[ZI> MnPMNlI5OjV|M{G=
PSN-1 NF\WUm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInvd3YxNjFzLUmg{txO Mn7TNUBp NW[2RYtTcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? MmjLNlI5OjV|M{G=

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:

[2]

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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:

[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 to the product individually and in order:
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
Formula

C18H16N4O3S

CAS No. 1232410-49-9
Storage powder
Synonyms N/A

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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).

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Dilution Calculator

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

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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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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