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Submit ReviewGeA-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.
分子量 | 300.35 |
公式 | C20H16N2O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2143475-98-1 |
PubChem ID | 135397654 |
InChI Key | LDPDVNYCIOHPGF-UHFFFAOYSA-N |
Smiles | O=C(NC=1C=CC=CC1C=2C=CC=C3C=4C=CC=CC4NC23)C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 30.03 | 100 | |
ethanol | 15.02 | 50 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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
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