2143475-98-1

GeA-69 is a cell-permeable, selective allosteric inhibitor targeting macrodomain 2 (MD2) of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14).

GeA-69 is a selective allosteric inhibitor of macrodomain 2 of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14)an anti-apoptotic pro-survival protein associated with inflammatory diseases and several types of cancer. GeA-69 exhibited a KD of 860 nM in ITC experiments. GeA-69 was shown to be an allosteric inhibitor of adenosine diphosphate ribose (ADPR) binding to PARP14 macrodomain 2 and to prevent recruitment of the PAPP14 macrodomain 2 to DNA damage sites.

PARP14: 2.1 μM (Kd)

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