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.
Cited by 19 Publications
6 Customer Reviews
Cell viability response to ATR inhibitor.
Nature, 2018, 555(7696):387-391. VE-821 purchased from Selleck.
ATM-repleted (GM16667) cells were pre-treated with inhibitors of ATM, ATR and DNA-PK (KU60019, VE-821 and NU-7441, respectively) for 1 h before subjecting cells to 10 Gy of irradiation. Cell lysates were harvested 1 h after irradiation. The result is representative of two independent experiments.
Blood Cancer J, 2016, 6(9):e465. 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.
Purity & Quality Control
Choose Selective ATM/ATR Inhibitors
|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.|
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.  VE-821 inhibits H2AX cell growth with IC50 of 800 nM. 
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
|In vitro||DMSO||74 mg/mL (200.86 mM)|
|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.
* 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.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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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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