ME0328

产品说明书

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Chemical Structure| 1445251-22-8 同义名 : -
CAS号 : 1445251-22-8
货号 : A562763
分子式 : C19H19N3O2
纯度 : 99%+
分子量 : 321.373
MDL号 : MFCD27991291
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 80 mg/mL(248.93 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PARP1

    PARP1, IC50:6.3 μM

  • PARP3

    PARP3, IC50:0.89 μM
描述 ME0328 is recognized as a potent and selective ARTD3/PARP3 inhibitor, active within cellular environments. It demonstrates an ability to inhibit ARTD3's transferase activity, with an IC50 of 0.89±0.28 μM, as determined by in vitro histone H1 modification assays. In A549 human cells, both ME0328 and ME0355, at a concentration of 10 μM, prolong the presence of γH2AX foci, indicative of a delay in DNA double-strand break repair post γ-irradiation of 2 Gy. ME0328 has been characterized through in silico and in vitro analyses to be soluble, capable of cell penetration, and metabolically stable in human liver microsomes and rat hepatocytes[1].
作用机制 ME0328 targets the nicotinamide binding site.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.11mL

0.62mL

0.31mL

15.56mL

3.11mL

1.56mL

31.12mL

6.22mL

3.11mL
参考文献

[1]Lindgren AE, et al. PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3. ACS Chem Biol. 2013 Aug 16;8(8):1698-703.