POB (Synonyms: N-(4′-Pyridoxyl)-L-Ornithine(BOC)-Ome) |
カタログ番号GB40328 |
POB(946135-39-3)は、ポリアミン合成に関与する主要な酵素であり、がん治療の潜在的な標的であるODCのプロドラッグ阻害剤である。細胞内では、POBはピリドキサルキナーゼによってリン酸化され、メチルエステルが加水分解されます。この活性化した阻害剤はおそらくapo-ODCに結合し、大幅にODC活性を低下させて細胞増殖を抑制します。 POBはLN229(IC50 = 50μM)、Jurkat、COS7、SW2および高・低グレードの多形性膠芽腫など多種多様な腫瘍細胞株の増殖を抑制することができました。DFMOよりも強力です。
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Cas No.: 946135-39-3
Sample solution is provided at 25 µL, 10mM.
POB (946135-39-3) is a transition state-based, cell permeable pro-drug inhibitor of ODC, a key enzyme involved in polyamine synthesis and a potential cancer drug target. Intracellularly, POB is phosphorylated by pyridoxal kinase and the methyl ester hydrolyzed. This active inhibitor most likely binds apo-ODC resulting in greatly reduced ODC activity and inhibition of cellular proliferation. POB was able to inhibit proliferation in a wide variety of tumor cell lines: LN229 (IC50 = 50 μM), Jurkat, COS7, SW2 and both high and low-grade glioblastoma multiforme. More potent than DFMO.
Average Rating: 5
(Based on Reviews and 30 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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