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MilliporeSigma™ Calbiochem™ ATR Inhibitor IV

A cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive ( K i = 13nM; IC50 /[ATP] = 70 nM/50µM and 128 nM/100µM), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs ( K

Manufacturer:  MilliporeSigma™ 5.04972.0001

Catalog No. 50-497-20001


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Description

Description

A cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive ( K i= 13nM; IC50/[ATP] = 70 nM/50µM and 128 nM/100µM), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs ( K i= 2.2, 3.9, 16, and >1µM, respectively, against DNA-PK, PI 3-Kγ, ATM, and mTOR) and 50 other kinases. Shown to selectively inhibit ATR-dependent H2AX Ser139 and Chk1 Ser345 phosphorylation (complete inhibition at 10µM in HT29 and HFL1 cultures) without affecting ATM- and DNA-PK-mediated H2AX or ATM-mediated Chk2 phosphorylation. Short-term (24 h) VE-821 treatment, either alone or in synergy with Cisplatin (Cat. No. 232120), results in reversible cytostatic growth arrest regardless of cellular ATM-p53 pathway activity, while cytotoxicity and Cisplatin synergism in cell death induction is reported to occur only upon long-term VE-821 exposure (≥72 h) in cultures with ATM-p53 pathway defects.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Specifications

Specifications

98% by HPLC
Protect from Light
ATR
368.41g/mol
Yellow solid
10mg
C18H16N4O3S
DMSO
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