• 产品描述： GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2 (MD2), with a Kd 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

• 靶点： PARP14:2.1 μM (Kd);PARP

• 体外研究：
  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. Cell Cytotoxicity Assay Cell Line: HeLa, U-2 OS and HEK293 cells Concentration: 25 nM-250 μM Incubation Time: 72 hours Result: Resulted moderate cytotoxicity against normal cells with EC50_HeLa=58 µM, EC50_U-2 OS=52 µM, EC50_HEK293=54 µM.

• 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.

• 溶解性： Soluble  in  DMSO

• 保存条件： 2-8°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.329 ml	16.647 ml	33.294 ml
  5 mM	0.666 ml	3.329 ml	6.659 ml
  10 mM	0.333 ml	1.665 ml	3.329 ml
  50 mM	0.067 ml	0.333 ml	0.666 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *