Q-VD-OPhCAS号: 1135695-98-5分子式: C26H25F2N3O6分子量: 513.49描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
Q-VD-OPh is a potent pan-caspase inhibitor with IC50 ranging from 25 to 400 nM for caspases 1, 3, 8, and 9, showing inhibitory effects on terminal caspase activation, substrate cleavage, and DNA ladder formation associated with apoptosis. |
纯度 |
>98%
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储存/保存方法 |
store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
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基本信息 | |
别名 |
QVD-OPH;Quinoline-Val-Asp-Difluorophenoxymethylketone
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外观 |
white to light brown powder
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可溶性/溶解性 |
DMSO : 100 mg/mL (194.75 mM; Need ultrasonic)
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生物活性 | |
靶点 |
Caspase
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In vitro(体外研究) |
Q-VD-OPh is a potent inhibitor of caspase-7 with an IC50 of 48 nM utilizing a cell-free assay consisting of human recombinant caspase-7, Q-VD-OPh, and the substrate AMC-DEVD-pNa. Q-VD-OPh fully inhibits caspase-3 and -7 activity at 0.05 μM. Caspase-8 is also inhibited at low Q-VD-OPh concentrations. The cleavage of PARP-1 is fully prevented at 10 μM Q-VD-OPh. DNA fragmentation and disruption of the cell membrane functionality are both prevented at 2 μM Q-VD-OPh. Q-VD-OPh is significantly more effective in preventing apoptosis than the widely used inhibitors, ZVAD-fmk and Boc-D-fmk, and is also equally effective in preventing apoptosis mediated by the three major apoptotic pathways, caspase 9/3, caspase 8/10, and caspase12. Q-VD-OPh is not toxic to cells even at extremely high concentrations. QVD is also able to increase the expression of differentiation markers in acute myeloid leukemia (AmL) blasts. QVD alone or combined with VDDs increases differentiation and HPK1-cJun signaling in AmL cell context-dependent manner.
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In vivo(体内研究) |
Chronic treatment with Q-VD-OPh prevents caspase-7 activation and limits the pathological changes associated with tau, including caspase cleavage. Q-VD-OPh could be a potential therapeutic compound for the treatment of Alzheimer’s disease.
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分子结构图