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GeA-69
- Soluble in DMSO
- MF: C20H16N2O
- MW: 300.35
Description
GeA-69 is a selective, allosteric and cell-active macrodomain inhibitor targeting macrodomain 2 of PARP14 (IC50 value of 0.71 µM). Moreover, GeA-69 engages PARP14 MD2 in intact cells and prevents its localisation to sites of DNA damage.
More Information
| Parent CAS No. | 2143475-98-1 |
|---|---|
| Chemical Name | N-(2-(9H-Carbazol-1-yl)phenyl)acetamide |
| SMILES | C1C=C2C3C=CC=C(C4C(NC(=O)C)=CC=CC=4)C=3NC2=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C20H16N2O/c1-13(23)21-18-11-4-2-7-14(18)16-9-6-10-17-15-8-3-5-12-19(15)22-20(16)17/h2-12,22H,1H3,(H,21,23) |
| InChiKey | LDPDVNYCIOHPGF-UHFFFAOYSA-N |
| CID | 135397654 |
| Short Description | PARP14 MD2 inhibitor |
References
- M Schuller et al. Discovery of a Selective Allosteric Inhibitor Targeting Macrodomain 2 of Polyadenosine-Diphosphate-Ribose Polymerase 14. ACS Chem Biol. 2017 Nov 17;12(11):2866-2874.
- M Moustakim et al. Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2. Bioorg Med Chem. 2018 Jul 15;26(11):2965-2972.
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