BYK204165

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Chemical Structure| 1104546-89-5 同义名 : PARP Inhibitor XIV
CAS号 : 1104546-89-5
货号 : A1219188
分子式 : C15H12N2O2
纯度 : 98%+
分子量 : 252.27
MDL号 : MFCD12912397
存储条件:

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Poly (ADP-ribose) polymerase (PARP) is a nuclear enzyme activated by strand breaks in DNA and implicated in DNA repair, apoptosis, organ dysfunction or necrosis. BYK204165, a potent and selective PARP1 inhibitor, inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 discriminates between PARP-1 and PARP-2 by a factor of 100 (pIC50 7.35 versus 5.38). Addition of BYK204165 (30 nM-3 μM) resulted in rightward shifts of the apparent Km value of NAD+[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.96mL

0.79mL

0.40mL

19.82mL

3.96mL

1.98mL

39.64mL

7.93mL

3.96mL

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):1587-1598