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BYK 204165

A selective inhibitor of PARP1

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BYK 204165的二维码
  • 库存: 现货
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  • 10mg
    ¥1787.00
    1430.00
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  • 50mg
    ¥7500.00
    6000.00
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  • 货号: ajci5622
  • CAS: 1104546-89-5
  • 别名: PARP Inhibitor XIV
  • 分子式: C15H12N2O2
  • 分子量: 252.27
  • 纯度: >98%
  • 溶解度: <25.23mg/ml in DMSO
  • 储存: Desiccate at 4°C
  • 库存: 现货

Background

BYK 204165 is a potent and selective poly(ADP-ribose) polymerase (PARP)-1 inhibitor with pIC50 values of 5.38 and 7.35 for PARP-2 and PARP-1 respectively [1].
PARP1 is a nuclear enzyme activated by strand breaks in DNA and involved in the regulation of various cell processes such as DNA repair, apoptosis, organ dysfunction or necrosis [1].
BYK 204165 (PARP inhibitor XIV) is a cell-permeable isoquinolinedione compound that potently and selectively inhibits PARP1. BYK 204165's potency is similar or higher than most current standard PARP-1 inhibitors (just slightly lower than PJ34), and it is 100-fold selective for PARP-1 over PARP-2 [1].
BYK 204165 was not tested in vivo because of BYK its poor water solubility.
参考文献:
[1]. Eltze T, Boer R, Wagner T, et al. Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors. Mol Pharmacol, 2008, 74(6): 1587-98.

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