PJ34 Hydrochloride

別包装 あり 純度 >=95% 分子量 331.8 CAS RN® 344458-15-7 化合物の概要 PARP inhibitor; potential Pim1 inhibitor. 構造 C17H17N3O2 HCl 溶媒 DMSO66 mg/mL (198.91 mM)Water66 mg/mL (198.91 mM)EthanolInsoluble 使用目的 PJ34 is a phenanthridinone derivative that acts as a competitive poly(ADP)-ribose polymerase (PARP) inhibitor. PJ34 exhibits cardioprotective, neuroprotective, anticancer, and anti-diabetic activities. In in vitro and in vivo models of oxygen glucose deprivation, PJ34 protects against stroke-related ischemic brain injury. This compound is also cardioprotective against myocardial infarction, decreasing infarct size and postsystolic shortening. In diabetic NOD mice, PJ34 decreased insulitis, beta-cell destruction, and diabetes incidence by decreasing islet IFN-γ expression and inducing apoptosis in islet-infiltrating leukocytes. In mouse models of allergic encephalitis, PJ34 exhibits protective benefit by shifting the immune response from a pro-inflammatory Th1-mediated response to an anti-inflammatory Th2-mediated response. Additionally, in a variety of cancer cell lines, PJ34 induces G2/M phase mitotic arrest and caspase-depedent apoptosis, potentially due to direct antagonism of Pim-1 kinase. 参考文献 Antolin AA, Jalencas X, Yelamos J, et al. Identification of pim kinases as novel targets for PJ34 with confounding effects in PARP biology. ACS Chem Biol. 2012 Dec 21;7(12):1962-7. PMID: 23025350.Gangopadhyay NN, Luketich JD, Opest A, et al. Inhibition of poly(ADP-ribose) polymerase (PARP) induces apoptosis in lung cancer cell lines. Cancer Invest. 2011 Nov;29(9):608-16. PMID: 22011283.Madison DL, Stauffer D, Lundblad JR. The PARP inhibitor PJ34 causes a PARP1-independent, p21 dependent mitotic arrest. DNA Repair (Amst). 2011 Oct 10;10(10):1003-13. PMID: 21840268.Scott GS, Kean RB, Mikheeva T, et al. 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. PMID: 15159442.Suarez-Pinzon WL, Mabley JG, Power R, et al. Poly (ADP-ribose) polymerase inhibition prevents spontaneous and recurrent autoimmune diabetes in NOD mice by inducing apoptosis of islet-infiltrating leukocytes. Diabetes. 2003 Jul;52(7):1683-8. PMID: 12829633.Faro R, Toyoda Y, McCully JD, et al. Myocardial protection by PJ34, a novel potent poly (ADP-ribose) synthetase inhibitor. Ann Thorac Surg. 2002 Feb;73(2):575-81. PMID: 11845877.Abdelkarim GE, Gertz K, Harms C, et al. Protective effects of PJ34, a novel, potent inhibitor of poly(ADP-ribose) polymerase (PARP) in in vitro and in vivo models of stroke. Int J Mol Med. 2001 Mar;7(3):255-60. PMID: 11179503.	メーカー 品番 包装 LKT P3600 25 MG 希望販売価格 ¥143,000 ※表示価格について 当社在庫 なし 納期目安 1週間程度 保存温度 -２０℃     メーカー情報 メーカー名 LKT Laboratories, Inc. 略号 LKT 関連情報 データシート 同等品検索
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