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| Cas No.: | 1135695-98-5 |
| SMILES: | CC(C)[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)COC1=C(C=CC=C1F)F)NC(=O)C2=NC3=CC=CC=C3C=C2 |
| Formula: | C26H25F2N3O6 |
| M.Wt: | 513.49 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Q-VD-OPha is a irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPha is able to cross the blood-brain barrier. |
| Target: | Caspase-3:25-400 nM (IC50) Caspase-7:48 nM (IC50) Caspase-1:25-400 nM (IC50) Caspase-8:25-400 nM (IC50) Caspase-9:25-400 nM (IC50) Caspase-10:25-400 nM (IC50) Caspase-12:25-400 nM (IC50) |
| In Vivo: | 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[1]. |
| In Vitro: | 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[1]. 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[2]. 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[3]. 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[4]. |
| Animal Administration: | Mouse: Stock solutions of Q-VD-OPh are prepared in DMSO and diluted in sterile PBS solution prior to injection. A final concentration of 10 mg/kg is chosen indicating neuroprotection at this concentration of Q-VD-OPh. Three-month old mice are divided into two groups: control, vehicle (n=3) or treated (n=2). Mice are injected i.p. three times a week with either Q-VD-OPh or vehicle for a total time period of 3 months[1]. |
| References: | [1]. Rohn TT, et al. Caspase activation in transgenic mice with Alzheimer-like pathology: results from a pilot study utilizing the caspase inhibitor, Q-VD-OPh. Int J Clin Exp Med. 2009 Nov 5;2(4):300-8. [2]. Kuzelová K, et al. Dose-dependent effects of the caspase inhibitor Q-VD-OPh on different apoptosis-related processes. J Cell Biochem. 2011 Nov;112(11):3334-42. [3]. Caserta TM, et al. Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties. Apoptosis. 2003 Aug;8(4):345-52. [4]. Chen-Deutsch X, et al. Leuk Res. 2012 Jul;36(7):884-8.The pan-caspase inhibitor Q-VD-OPh has anti-leukemia effects and can interact with vitamin D analogs to increase HPK1 signaling in AML cells. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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