化合物 PJ34|T6197|TargetMol

PJ34
344458-19-1

￥464 10mg 起订

￥874 25mg 起订

￥1410 50mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 PJ34

英文名称：: PJ34

CAS号：: 344458-19-1

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.85%

产品类别：: 抑制剂

货号：: T6197

Product Introduction

Bioactivity

名称	PJ34
描述	PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.
细胞实验	PJ34 is dissolved in 100% DMSO at 10 mM and then diluted in DMEM without serum[1]. PC12 cell cultured are grown in Dulbecco's modified Eagle's medium supplemented with 5% (v/v) fetal calf serum, 5% (v/v) horse serum, and a 1% (v/v) penicillin-streptomycin antibiotics mixture. Cells are grown in an atmosphere of 95% air and 5% CO2 at 37°C. For all experiment, cells are seeded at a density of 4×104 cells/well in 96-well culture plates and allowed to attach overnight. For assessment of cell viability, hydrogen peroxide-induced cytotoxicity is quantified by a standard measurement of LDH release with the use of the LDH assay kit. Briefly, 6 h after hydrogen peroxide exposure, 20 μL of medium of each well is collected, and the solution prepared from LDH assay kit is added. After incubation at room temperature for 30 min, the reaction is stopped by addition of 1 N HCl, and absorbance is measured at 450 nm using a microplate reader.
激酶实验	To assess the PARP-1 or PARP-2 inhibitory activity of FR247304, 3-AB, and PJ34, PARP activity is evaluated with minor modifications. PARP enzyme assay is carried out in a final volume of 100 μL consisting of 50 mM Tris-HCl (pH 8.0), 25 mM MgCl2, 1 mM dithiothreitol, 10 μg activated salmon sperm DNA, 0.1 μCi of [adenylate-32P]NAD, 0.2 units of recombinant human PARP for PARP-1 assay or 0.1 units of recombinant mouse PARP-2 for PARP-2 assay, and various concentrations of FR261529 or 3-AB. The reaction mixture is incubated at room temperature (23°C) for 15 min, and the reaction is terminated by adding 200 μL of ice-cold 20% trichloroacetic acid (TCA) and incubated at 4°C for 10 min. The precipitate is transferred onto GF/B filter and washed three times with 10% TCA solution and 70% ethanol. After the filter is dried, the radioactivity is determined by liquid scintillation counting.
体外活性	PJ34通过抑制PARP酶活性，其IC50值为110±1.9 nM。通过LDH测定法评估PJ34与其他PARP抑制剂在PC12细胞中的神经保护性能，比较结果表明，PJ34在从10-7到10-5 M范围内的浓度下，显著并且依赖浓度地减少细胞死亡[1]。
体内活性	为了与其他PARP抑制剂进行效能及功效的比较，评估PJ34的剂量分别为3.2和10 mg/kg。3.2 mg/kg的剂量显著降低了皮质损伤33%，而10 mg/kg的剂量则显示出相反效果（降低了17%）[1]。25 mg/kg的PJ34能够将缺血动物的TNF-α mRNA水平降低70%，且这些数值与假手术或未处理动物无差异。PJ34对缺血小鼠的治疗降低了E-selectin mRNA的水平81%，ICAM-1 mRNA的水平降低了54%，与仅接受载体处理的缺血小鼠相比[2]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 2.95 mg/mL (10 mM)
关键字	Inhibitor \| PARP \| PJ-34 \| inhibit \| PJ34 \| PJ 34 \| poly ADP ribose polymerase
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PJ34|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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