| Identification | Back Directory | [Name]
SU-11752 | [CAS]
688036-19-3 | [Synonyms]
SU-11752
1H-Pyrrole-3-propanoic acid, 5-[[1,2-dihydro-2-oxo-5-[(phenylamino)sulfonyl]-3H-indol-3-ylidene]methyl]-2,4-diethyl- | [Molecular Formula]
C26H27N3O5S | [MOL File]
688036-19-3.mol | [Molecular Weight]
493.57 |
| Hazard Information | Back Directory | [Description]
SU-11752 is a potent and selective DNA-PK inhibitor. Inhibition kinetics and a direct assay for ATP binding showed that SU11752 inhibited DNA-PK by competing with ATP. SU11752 inhibited DNA double-strand break repair in cells and gave rise to a five-fold sensitization to ionizing radiation. At concentrations of SU11752 that inhibited DNA repair, cell cycle progression was still normal and ATM kinase activity was not inhibited. | [Uses]
SU-11752 is an inhibitor for DNA-dependent protein kinase (DNA-PK) with an IC50 of 0.13 μM. SU-11752 inhibits PI3K p110γ kinase with IC50 of 1.1 μM. SU-11752 binds competitively for ATP-site in DNA-PK, results in inhibition of intracellular DNA double-strand break repair and increases the sensitivity of cells to radiotherapy[1]. | [IC 50]
DNA-PK: 0.13 μM (IC50); p110γ: 1.1 μM (IC50) | [References]
[1] Ismail IH, et al., SU11752 inhibits the DNA-dependent protein kinase and DNA double-strand break repair resulting in ionizing radiation sensitization. Oncogene. 2004 Jan 29;23(4):873-82. DOI:10.1038/sj.onc.1207303 |
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