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BYK204165

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BYK204165  纯度: 99.68%

BYK204165 是一种有效的选择性 PARP1 抑制剂。BYK204165 抑制重组人 PARP-1 (hPARP-1)，pIC50 值为 7.35 (pKi 7.05)。抑制鼠 PARP-2 (mPARP-2)，pIC50 值为 5.38 。BYK204165 对 PARP-1 的选择性比对 PARP-2 高 100 倍。

BYK204165

BYK204165 Chemical Structure

CAS No. : 1104546-89-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1160 In-stock
5 mg ￥1050 In-stock
10 mg ￥1650 In-stock
50 mg ￥6950 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 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 displays 100-fold selectivity for PARP-1[1].

IC50 & Target[1]

hPARP-1

7.35 (pIC50)

mPARP-2

5.38 (pIC50)

体外研究
(In Vitro)

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

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

BYK204165 is not investigated in vivo because of its short half-time (t1/2) of 23 min measured at rat microsomes in vitro[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

252.27

Formula

C15H12N2O2
CAS 号

1104546-89-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (495.50 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9640 mL 19.8200 mL 39.6401 mL
5 mM 0.7928 mL 3.9640 mL 7.9280 mL
10 mM 0.3964 mL 1.9820 mL 3.9640 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [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.

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