Q-VD-OPh 是一种不可逆的泛胱天蛋白酶 (caspase) 抑制剂，具有高效的抗凋亡能力。抑制胱天蛋白酶 7 的 IC50 值别为 48 nM，抑制胱天蛋白酶 1，3，8，9，10，12 的 IC50 值在 25-400 nM 之间。Q-VD-OPh 可抑制 HIV 感染。Q-VD-OPh 能透过血脑屏障。
| CAS No. | 1135695-98-5 |
| 生物活性 | Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier. |
| 分子式 | C26H25N3O6F2 |
| 分子量 | 513.49 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : 100 mg/mL (194.75 mM; Need ultrasonic) |
| 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. |
| 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. |
| 文献 | •Cell Mol Immunol. 2021 May;18(5):1186-1196. •Br J Pharmacol. 2021 Jul 7. •Cell Death Dis. 2020 Apr 24;11(4):281. •Antioxid Redox Signal. 2021 Dec 16. •J Med Chem. 2021 Feb 4. •Cancer Sci. 2019 May;110(5):1746-1759. •Ecotoxicol Environ Saf. November 2021, 112632. •Commun Biol. 2021 Mar 5;4(1):291. •Biochem Pharmacol. 2021 Jan;183:114352. •J Cell Sci. 2019 Feb 28;132(5). •Transl Oncol. November 2021, 101203. •Immunol Cell Biol. 2021 Jan;99(1):34-48. •Calcif Tissue Int. 2020 Nov;107(5):499-509. •J Orthop Surg Res. 2019 Dec 17;14(1):448. •Mol Biol Rep. 2020 Apr;47(4):2713-2722. •McGill University. Integrated Program in Neuroscience. 2021 Dec. •St. Johns University. 2021 Jul. •bioRxiv. 2021 Jan 15. •Cell Physiol Biochem. 2017;42(5):1822-1836. |
| 纯度及产品资料 | 98% |
邮箱：info@TianyaBio.com
电话：020-3107 8154
地址：广州市番禺区兴业大道东路1078号2-50
微信公众号
微信客服
