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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.
Selective allosteric inhibitor of PARP14 macrodomain 2
| assay | ≥98% (HPLC) |
| form | powder |
| color | off-white to brown |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | CC(NC1=CC=CC=C1C2=CC=CC3=C2NC4=CC=CC=C43)=O |
| InChI key | LDPDVNYCIOHPGF-UHFFFAOYSA-N |
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¥ 1148.92
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¥ 1573.49
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¥ 1779.22
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¥ 6330.00
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¥ 14407.09
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¥ 1196.00
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¥ 1749.15
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¥ 2869.87
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