|BYK 204165PARP-1 inhibitor,potent and selective|
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||1104546-89-5||SDF||Download SDF|
|Solubility||Soluble in DMSO > 10 mM||Storage||Desiccate at 4°C|
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 .
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 .
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 .
BYK 204165 was not tested in vivo because of BYK its poor water solubility.
. 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.