Biochem/physiol Actions
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.
| Colour | off-white to brown |
|---|---|
| Manufacturer | SIGMA-ALDRICH |
| Storage Temp. | 2-8°C |
| Solubility | DMSO: 2 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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