1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. PARP-2/1-IN-2

PARP-2/1-IN-2  (Synonyms: ABT-888对映体)

目录号: HY-105253
产品使用指南

PARP-2/1-IN-2 (Compound 4a) 是 Veliparib (HY-10129) 的对映异构体,是一种有效的 PARP 抑制剂,对 PARP-2PARP-1Ki 分别为 2 和 5 nM。在以 PARP 活性为基础的细胞测定中,PARP-2/1-IN-2 的 EC50 为 3 nM。

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PARP-2/1-IN-2 Chemical Structure

PARP-2/1-IN-2 Chemical Structure

CAS No. : 912444-01-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PARP-2/1-IN-2 (Compound 4a), the enantiomer of Veliparib (HY-10129), is a potent PARP inhibitor with Kis of 2 and 5 nM against PARP-2 and PARP-1, respectively. PARP-2/1-IN-2 has an EC50 of 3 nM in a cell based assay of PARP activity[1].

IC50 & Target[1]

PARP2

2 nM (Ki)

PARP1

5 nM (Ki)

体内研究
(In Vivo)

PARP-2/1-IN-2 (Compound 4a) (25 or 50 mg/kg; i.p.) 在 Cisplatin (HY-17394) 和 Oxaliplatin (HY-17371) 诱导的小鼠神经病变中减轻疼痛[1]

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

Animal Model: Male C57BL6J mice, Cisplatin (HY-17394) and Oxaliplatin (HY-17371)-induced painful neuropathy models[1]
Dosage: 25 mg/kg or 50 mg/kg
Administration: Intraperitoneal injection, two days prior to treatment with Cisplatin or oxaliplatin, with administration continuing by i.p. injection along with the Cisplatin or oxaliplatin regimen (5 days, followed by 5 days of rest, for two weekly cycles)
Result: Does not attenuate Cisplatin and Oxaliplatin-induced body weight loss. Does not Affect the decline in exploratory behavior associated with Cisplatin and Oxaliplatin Treatment. Attenuates mechanical allodynia in Cisplatin and Oxaliplatin-induced neuropathy. Attenuates thermal hyperalgesia in Cisplatin-induced neuropathy. Attenuates cold hyperalgesia associated with Oxaliplatin-induced neuropathy.
分子量

244.29

Formula

C13H16N4O

CAS 号
中文名称

ABT-888对映体

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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PARP-2/1-IN-2
目录号:
HY-105253
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