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Biological Activity:

ME0328 is a potent, selective and cell permeable PARP-3 inhibitor with IC50 of 0.89 μM. It has good selectivity against PARP-1, PARP-2 and other ARDT enzymes. Enhances CRISPR-Cas9-mediated HER2 mutation frequency, resulting in increased reduction in proliferation of HER2-positive breast cancer cells.

How to Use:

In vitro: ME0328 was used at 10 µM in vitro and cellular assays.
In vivo: n/a

Reference:

• 1. Lindgren AE, et al. PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3. (2013) ACS Chem Biol. 8(8):1698-703. 
• 2. Wang H, et al. CRISPR-mediated targeting of HER2 inhibits cell proliferation through a dominant negative mutation. (2017) Cancer Lett. 385:137-143. 
• 3. Day TA, et al. PARP3 is a promoter of chromosomal rearrangements and limits G4 DNA. (2017) Nat Commun. 8:15110.