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Background: PAR homeostasis is regulated by the family of PAR polymerases (PARPs) and PARG (Poly (ADP-ribose) glycohydrolase) in response to cellular stress conditions. ADP ribosylation, which is the addition of an ADP-ribose to a protein, is a reversible post-translational modification of proteins mostly involved in the DNA Damage Response (DDR) pathway. Poly-ADP-ribosylation (termed PARylation) is the addition of linear or branched chains of ADP-ribose. PARP and PARG activity are linked to cellular responses in inflammation, ischemia, stroke, and cancer. PARP inhibitors have been used in cancer treatment with success, leading to synthetic lethality when homologous recombination repair (HRR) is already defective. PARG is overexpressed in breast cancer and associated with tumor growth and survival. Decrease in PARG activity can potentiate the effect of current cancer therapies, such as chemotherapy and radiation, making PARG inhibition with selective inhibitors a promising approach in cancer and immunotherapy. Further studies of PARP and PARG will elucidate how the levels of PARylated proteins contribute to disease and can be modulated to provide therapeutic benefit.
CAS Number: 763113-22-0,1207456-01-6,284028-89-3,2381037-82-5,2360851-29-0,1945950-21-9
Description: The Complete ADP-Ribosylation Cycle Inhibitor Cocktail is a mixture of selected highly selective ADP-ribosylation cycle inhibitors and broad specificity inhibitors. This product contains five ADP-ribosylation cycle inhibitors of Poly (ADP-ribose) polymerase (PARP) isozymes such as Olaparib, Talazoparib, XAV-939, RBN-2397, RBN-012759, and one potent, selective poly (ADP-ribose) glycohydrolase/PARG inhibitor, PDD00017273. Used all together, these inhibitors "freeze" the state of cellular ribosylation at the time the mix is applied to the cells. This product is designed to supplement a cell lysis buffer of choice to prevent post-lysis changes in the ADP-ribosylation status of extracted proteins.
Formulation: 5 mM AZD2281 (Olaparib) (#27003), 500 µM PDD00017273, 50 µM XAV-939 (#27100), 50 µM RBN-2397, 50 µM RBN-012759, and 500 µM Talazoparib.
Storage Stability: Upon receipt freeze (-80°C). Stable for 6 months from date of receipt, when stored as directed.
Warnings: Avoid freeze/thaw cycle
Biosafety Level: Not applicable (BSL-1)
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