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Description: Selective allosteric PARP14 inhibitor
Chemical Name: N-[2-(9H-Carbazol-1-yl)phenyl]acetamide
Purity: ≥98% (HPLC)
Literature (2)

Biological Activity for GeA-69

GeA-69 is a selective allosteric inhibitor of poly (ADP-ribose) polymerase 14 (PARP14) macrodomain 2 (MD2) (IC50 = 720 nM, Kd = 860 nM). It inhibits adenosine diphosphate ribose (ADPR) binding to the macrodomain 2 of PARP14 and prevents PARP14 MD2 localization to DNA damage sites in intact cells. GeA-69 is highly cell permeable.

Technical Data for GeA-69

M. Wt 300.35
Formula C20H16N2O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2143475-98-1
PubChem ID 135397654
Smiles O=C(NC=1C=CC=CC1C=2C=CC=C3C=4C=CC=CC4NC23)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GeA-69

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 30.03 100
ethanol 15.02 50

Preparing Stock Solutions for GeA-69

The following data is based on the product molecular weight 300.35. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.33 mL 16.65 mL 33.29 mL
5 mM 0.67 mL 3.33 mL 6.66 mL
10 mM 0.33 mL 1.66 mL 3.33 mL
50 mM 0.07 mL 0.33 mL 0.67 mL

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References for GeA-69

References are publications that support the biological activity of the product.

Schuller et al (2017) Discovery of a selective allosteric inhibitor targeting macrodomain 2 of polyadenosine-diphosphate-ribose polymerase 14. ACS Chem.Biol. 12 2866 PMID: 28991428

Moustakim et al (2018) Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2. Bioorg.Med.Chem. 26 2965 PMID: 29567296

If you know of a relevant reference for GeA-69, please let us know.

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Citations for GeA-69

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