PJ34

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PJ34

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

344458-19-1

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议

产品介绍

化学性质

Storage	Store at -20°C
M.Wt	295.34
Cas No.	344458-19-1
Formula	C₁₇H₁₇N₃O₂
Synonyms	PJ-34;PJ 34
Solubility	Soluble in DMSO
Chemical Name	2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide
Canonical SMILES	CN(C)CC(=O)NC1=CC2=C(C=C1)NC(=O)C3=CC=CC=C32
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

IC50 Value: 20 nM(EC50)[1] PJ34 (hydrochloride) is a novel potent specific inhibitor of PARP-l. PJ34 has been reported to enhance chemotherapeutic effects in certain types of tumors. in vitro: PJ34 inhibited peroxynitrite-induced cell necrosis with EC50 of 20 nM. PJ34 provides cardioprotection by decreasing myocardial infarct size and enhancing postischemic regional and global functional recovery [1]. Treatment with PJ34 increased NIS promoter activity without affecting PARP-1 binding to the promoter sequence, in addition to an increase of histone modification activation marks (H3K9K14ac, H3K4me3) [2]. in vivo: In a model of systemic endotoxemia, PJ34 pretreatment significantly reduced plasma levels of TNF-alpha, IL-1beta and nitrite/nitrate (breakdown products of nitric oxide) production. PJ34 treatment (oral gavage) induced a significant suppression of the inflammatory response in dextran sulfate colitis, multiple low dose streptozotocin diabetes [3]. The PJ34 showed significant reduction on infarct size (37.5%+/-4.5% and 50.5%+/-4.8% of the area at risk) for PJ34 and control pigs groups, respectively, (p < 0.05) [4]. Clinical trial: N/A

试验操作

细胞实验 [1]:
细胞系	小鼠内皮细胞和人脐静脉内皮细胞
制备方法	在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。
反应条件	0.1 ~ 3 μM
实验结果	在小鼠内皮细胞中，PJ34在0.5 μM和3 μM的剂量下显著抑制高浓度葡萄糖诱导的PARP活化，在3 μM的剂量下还能显著抑制高浓度葡萄糖诱导的内皮功能障碍发展。同时，由PJ34 (3 μM) 诱导的PARP抑制不会改变NF-κB活化程度。在人脐静脉内皮细胞中，1 μM PJ34对高浓度葡萄糖诱导的PARP活化具有显著的抑制作用。
动物实验 [2]:
动物模型	接受MBP免疫接种的PLSJL小鼠
给药剂量	10 mg/kg；口服给药；每天2次
实验结果	在接受MBP免疫接种的PLSJL小鼠中，PJ34抑制实验性过敏性脑脊髓炎 (EAE) 的临床体征发展。PJ34还减少了CNS炎症，维持神经血管完整性，从而抑制EAE发作。此外，PJ34下调脊髓组织TNF-α和ICAM-1的表达水平。
注意事项	请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。
References: [1]. Garcia Soriano F, Virág L, Jagtap P, Szabó E, Mabley JG, Liaudet L, Marton A, Hoyt DG, Murthy KG, Salzman AL, Southan GJ, Szabó C. Diabetic endothelial dysfunction: the role of poly(ADP-ribose) polymerase activation. Nat Med. 2001 Jan;7(1):108-13. [2]. Scott GS, Kean RB, Mikheeva T, Fabis MJ, Mabley JG, Szabó C, Hooper DC. The therapeutic effects of PJ34 [N-(6-oxo-5,6-dihydrophenanthridin-2-yl)-N,N-dimethylacetamide.HCl], a selective inhibitor of poly(ADP-ribose) polymerase, in experimental allergic encephalomyelitis are associated with immunomodulation. J Pharmacol Exp Ther. 2004 Sep;310(3):1053-61.

生物活性

PJ34 is a novel potent specific inhibitor of PARP-l/2 with EC50 of 20 nM.
Targets	PARP
IC50	20 nM (EC50)