生物活性 | |||
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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 | |||
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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 |
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