PARP inhibitors
PARP inhibitors
Poly (ADP-ribose) polymerase (PARP) inhibitors represent a class of therapeutic agents employed in the management of cancer, neurodegenerative disorders, and cardiovascular diseases. PARP enzymes play a critical role in repairing single-strand DNA breaks. When their activity is blocked, these lesions accumulate and convert into double-strand breaks during the rapid DNA replication typical of many malignancies and disease states.
Because these double-strand breaks can build up faster than cells are able to repair them, the result is often cell death. By contrast, normal cells usually replicate more slowly, allowing time for repair through alternative pathways such as homologous recombination, which makes them more resilient to PARP inhibition.
Certain tumor types are especially reliant on PARP function, making them highly susceptible to this therapeutic strategy. Beyond established applications in breast and pancreatic cancer, PARP inhibitors are also being investigated for their potential in brain tumors such as glioma and medulloblastoma.
· For instance, 3-Aminobenzamide (A107207 ≥98%, A408534 10mM in DMSO) enhances the potency of co-administered chemotherapeutics in glioma cell models.
· Veliparib (V127105≥99%, V408786 10mM in DMSO ) has been shown to reduce tumor progression when used in combination with the alkylating agent Temozolomide (T127425 ≥98%, T408143 10mM in DMSO), compared to Temozolomide alone.
· Additionally, Olaparib (O126162 ≥98%, O408041 10mM in DMSO ) has demonstrated the ability to sensitize multiple tumor cell lines—including ependymoma, glioma, and medulloblastoma—to radiation therapy.
Other PARP inhibitors available from Aladdin include AZD2461 (A127274 ≥98%, A408089 10mM in DMSO) and PJ34 Hydrochloride (P129886 ≥97%, P423512 10mM in DMSO).
References:
1. Piskunova TS, Yuorva MN, Ovsyannikov AI et al. Curr Gerontol Geriatr Res. 2008:754190.
2. Cheng CL, Johnson SP, Keir ST, et al. Mol Cancer Ther. 2005 Sep;4(9):1364-8.
3. van Vuurden DG, Hulleman E, Meijer OL, et al. Oncotarget. 2011 Dec;2(12):984-96.
4. Donawho CK, Luo Y, Luo Y, et al. Clin Cancer Res. 2007 May 1;13(9):2728-37.
Aladdin: https://www.aladdinsci.com/