MilliporeSigma™ Calbiochem™ ATR Inhibitor IV

Catalog No.	Quantity
50-497-20001	10 mg

Catalog No. 50-497-20001 Supplier MilliporeSigma™ Supplier No. 5049720001

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

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

• Color: Yellow
• Description: 98% by HPLC
• Target Proteins: ATR
• Molecular Formula: C₁₈H₁₆N₄O₃S
• Formula Weight: 368.41g/mol
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Solid
• Quantity: 10 mg