BYK 204165 是一种有效的选择性 PARP1 抑制剂。 BYK 204165 抑制无细胞重组人 PARP-1 (hPARP-1) 的 pIC50 为 7.35 (pKi\u003d7.05) 和鼠 PARP-2 (mPARP-2) 的 pIC50 分别为 5.38。 BYK 204165 对 PARP-1 的选择性提高了 100 倍。
| Cas No. | 1104546-89-5 |
| 化学名 | (4E)-4-[(1-methylpyrrol-2-yl)methylidene]isoquinoline-1,3-dione |
| Canonical SMILES | CN1C=CC=C1C=C2C3=CC=CC=C3C(=O)NC2=O |
| 分子式 | C15H12N2O2 |
| 分子量 | 252.27 |
| 溶解度 | <25.23mg/ml in DMSO |
| 储存条件 | Desiccate at 4℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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.
References:
[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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