GeA-69
目录号: PL08908 纯度: ≥99%
CAS No. :2143475-98-1
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中文名称
GeA-69
英文名称
GeA-69
英文别名
GeA69; GeA 69;BCP31007;N-(2-(9H-Carbazol-1-yl)phenyl)acetamide;N-[2-(9H-Carbazol-1-yl)phenyl]acetamide;GeA-69
Cas No.
2143475-98-1
分子式
C20H16N2O
分子量
300.35
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
GeA-69 是一种选择性的 PARP14 变构抑制剂,靶向作用于 macrodomain 2 (MD2),Kd 值为 2.1 µM。GeA-69 参与 DNA 损伤修复机制,能够防止 PARP14 MD2 募集到激光诱导的 DNA 损伤部位。
生物活性
GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2 (MD2), with a K d value of 2.1 μM. GeA-69 involves in DNA damage repair mechanisms and prevents recruitment of PARP14 MD2 to sites of laser-induced DNA damage.
性状
Solid
IC50 & Target[1][2]
PARP14 2.1 μM (Kd)
体外研究(In Vitro)
GeA-69 (compound 1) (50 μM and 250 μM; pre-damage for 1 h or 0.5, 1, 2.5 min) engages PARP14 MD2 in intact cells and prevents its localisation to sites of DNA damage in U-2 OS cells.
GeA-69 (25 nM-250 μM; 72 h) exhibits moderate cytotoxicity among HeLa, U-2 OS and HEK293 cells and highly cell permeable with 2 % passing paracellular and 98 % transcellular over the membrane.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Schuller M, 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.
[2]. Moustakim M, 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.
溶解度数据
In Vitro: DMSO : ≥ 125 mg/mL (416.18 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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