ETP-46464 (Synonyms: ATM Inhibitor III, ATR Inhibitor III) |
Catalog No.GC10196 |
ATR inhibitor,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1345675-02-6
Sample solution is provided at 25 µL, 10mM.
ETP-46464 is a potent and selective inhibitor for ATR (IC50 = 25 nM).
ATR (ATM- and Rad3-related) is a member of PIKK (phosphatidylinositol 3-kinase-like kinases) that regulates the DNA damage response pathways. It is a DNA damage sensor that is activated upon genotoxic stresses (e.g. ionizing radiation, UV radiation and DNA replication stalling) and phosphorylates its downstream substrates (e.g. p53, BRCA1 and CHEK1).
ETP-46464 abolished the G2/M checkpoint. It caused the presence of micronuclei or completely fragmented nuclei in cells under ionizing radiation. Cells treated simultaneously with hydroxyurea and ETP-46464 exhibited elevated ATM and Chk2 phosphorylation. In U2OS cells, ETP-46464 promoted the breakage of stalked replication forks. [1]
Reference:
1. Toledo LI, Murga M, Zur R et al. A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations. Nat Struct Mol Biol. 2011 Jun;18(6):721-7.
Average Rating: 5
(Based on Reviews and 32 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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