货号	规格	价格	上海	北京	珠海	重庆	武汉
S88582-5mg促销	98.80%	￥170.00 ￥136.00 S88582-5mg ￥136.00 现货	6 6	-	-	-	-
S88582-10mg促销	98.80%	￥270.00 ￥216.00 S88582-10mg ￥216.00 现货	7 7	-	-	-	-
S88582-25mg促销	98.80%	￥550.00 ￥440.00 S88582-25mg ￥440.00 现货	6 6	-	-	-	-
S88582-50mg促销	≥98%	￥730.00 ￥656.00 S88582-50mg ￥656.00 2-3天	0 货期：2-3天	-	-	-	-
S88582-100mg	≥98%	￥1030.00 S88582-100mg ￥1030.00 2-3天	0 货期：2-3天	-	-	-	-

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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。

参考文献

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