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PJ34 盐酸

高效的选择性PARP-1抑制剂
规格或纯度: ≥97%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
P129886-1mg
1mg 期货 Stock Image
P129886-5mg
5mg 现货 Stock Image
P129886-25mg
25mg 现货 Stock Image
P129886-100mg
100mg 现货 Stock Image

基本描述

别名 PJ 34 盐酸盐
英文别名 A874967|AS-72775|HY-13688|n-(6-oxo-5,6-dihydro-phenanthridin-2-yl)-n,n-dimethylacetamide hydrochloride|AKOS006340934|CCG-267823|N~2~,N~2~-Dimethyl-N-(6-oxo-5,6-dihydrophenanthridin-2-yl)glycinamide--hydrogen chloride (1/1)|EINECS 230-308-2|N(2),N(2)-dimet
规格或纯度 ≥97%
英文名称 PJ34 HCl
生化机理 PARP Inhibitor VIII, PJ34 is a cell-permeable, water-soluble phenanthridinone derivative which inhibits of poly(ADP-ribose) polymerase (PARP; EC50 = 20 nM). It is believed to be up to 10,000 times more potent than 3-aminobenzamide which has an EC = 200 μM. Studies have shown that PARP over-activation can lead to NAD depletion and consequent necrosis, thus inducing inflammatory conditions in many diseases. It has been observed that at lower concentrations, PARP Inhibitor VIII, PJ34 displays antioxidant activity. Studies conducted in vitro on stroke models indicate that this compound has neuroprotective functions. PARP Inhibitor VIII, PJ34 is an inhibitor of PARP-1 and PARP-2.Potent, selective PARP-1 inhibitor (EC 50 = 20 nM). Able to reduce both cell injury induced following deprivation of oxygen-glucose in vitro and infarct size following focal cerebral ischemia in vivo .
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

PJ34 HCl 是PJ34的盐酸盐形式,是一种PARP抑制剂,EC50为20 nM,同等有效作用于PARP1/2。

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.

名称和标识符

IUPAC Name 2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide;hydrochloride
INCHI InChI=1S/C17H17N3O2.ClH/c1-20(2)10-16(21)18-11-7-8-15-14(9-11)12-5-3-4-6-13(12)17(22)19-15;/h3-9H,10H2,1-2H3,(H,18,21)(H,19,22);1H
InChi Key RURAZZMDMNRXMI-UHFFFAOYSA-N
Canonical SMILES CN(C)CC(=O)NC1=CC2=C(C=C1)NC(=O)C3=CC=CC=C32.Cl
Isomeric SMILES CN(C)CC(=O)NC1=CC2=C(C=C1)NC(=O)C3=CC=CC=C32.Cl
WGK Germany 3
PubChem CID 16760621
分子量 331.8

化学和物理性质

溶解性 DMSO 66 mg/mL Water 66 mg/mL Ethanol

安全和危险性(GHS)

WGK Germany 3
个人防护装备 Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter

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参考文献

1. Schultz MB et al..  (2018)  Assays for NAD+-Dependent Reactions and NAD+ Metabolites..  Methods Mol Biol,  1813  ():  (77-90).  [PMID:30097862]
2. Liu P & Pan Q.  (2022)  Butein Inhibits Oxidative Stress Injury in Rats with Chronic Heart Failure via ERK/Nrf2 Signaling..  Cardiovasc Ther,  2022  ():  (8684014).  [PMID:35069800]
3. Robu M et al..  (2020)  Methods to Study Intracellular Movement and Localization of the Nucleotide Excision Repair Proteins at the DNA Lesions in Mammalian Cells..  Front Cell Dev Biol,  ():  (590242).  [PMID:33282869]
4. Martinerie C et al..  (2016)  NOV/CCN3: A New Adipocytokine Involved in Obesity-Associated Insulin Resistance..  Diabetes,  65  (9):  (2502-15).  [PMID:27284105]
5. Gupte R et al..  (2021)  Nuclear ADP-ribosylation drives IFN?-dependent STAT1a enhancer formation in macrophages..  Nat Commun,  12  ():  (3931).  [PMID:34168143]
6. Nilson KA et al..  (2017)  Oxidative stress rapidly stabilizes promoter-proximal paused Pol II across the human genome..  Nucleic Acids Res,  45  (19):  (11088-11105).  [PMID:28977633]
7. Bai XT et al..  (2015)  Small PARP inhibitor PJ-34 induces cell cycle arrest and apoptosis of adult T-cell leukemia cells..  J Hematol Oncol,  ():  (117).  [PMID:26497583]