BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC₅₀ of 7.35 (pK_i=7.05), and murine PARP-2 (mPARP-2) with a pIC₅₀ of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1.

Solid

In kinetic experiments with human PARP-1, BYK204165 exhibits potent and competitive inhibition of enzyme activity, yielding a pK_i value of 7.05.
BYK204165 exhibits low potency of PARP inhibition in C4I cells (pIC₅₀ of 5.75).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

BYK204165 is not investigated in vivo because of its short half-time (t_1/2) of 23 min measured at rat microsomes 体外研究.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature or refrigerated transportation.

• [1]. Eltze 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 Dec;74(6):1587-98.  [Information]

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。