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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
|Storage||Store at -20°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|
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.
|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|
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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Keywords: GeA-69, GeA-69 supplier, GeA69, GeA, 69, PARP, inhibitors, inhibits, PolyADP, ribose, Polymerases, Poly(ADP, ribose), Polymerase, adenosine, diphosphate, ADPR, selective, MD2, macrodomain, 2, Poly(ADP-ribose), 6795, Tocris Bioscience
Citations for GeA-69
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 170 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.