For research use only. Not for therapeutic Use.
AZ9482 is a triple PARP1/2/6 inhibitor, with IC50 values of 1 nM, 1 nM and 640 nM for PARP1, PARP2 and PARP6, respectively[1].
AZ9482 exhibits an EC50 of 24 nM in MDA-MB-468 cells[1].
AZ0108 treatment prevents CHK1 MARylation and induces hyperphosphorylation of CHK1, contributing to MPS formation and dysregulation of the cell cycle[1].
AZ0108 also displays toxicity in vivo, the molecular basis of which is currently undefined, limiting pharmacological evaluation of AZ0108[1].
| Catalog Number | I003498 |
| CAS Number | 1825345-33-2 |
| Synonyms | 2-[4-[3-[(4-oxo-3H-phthalazin-1-yl)methyl]benzoyl]piperazin-1-yl]pyridine-3-carbonitrile |
| Molecular Formula | C26H22N6O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C26H22N6O2/c27-17-20-7-4-10-28-24(20)31-11-13-32(14-12-31)26(34)19-6-3-5-18(15-19)16-23-21-8-1-2-9-22(21)25(33)30-29-23/h1-10,15H,11-14,16H2,(H,30,33) |
| InChIKey | ZDDPBFWHZOJFHF-UHFFFAOYSA-N |
| SMILES | C1CN(CCN1C2=C(C=CC=N2)C#N)C(=O)C3=CC=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54 |
| Reference | [1]. Ryan T Howard, et al. Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors. ACS Chem Biol. 2020 Feb 21;15(2):325-333. |
