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Q-VD-OPh

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Chemical Structure| 1135695-98-5 同义名 : Quinoline-Val-Asp-Difluorophenoxymethylketone
CAS号 : 1135695-98-5
货号 : A148116
分子式 : C26H25F2N3O6
纯度 : 97%
分子量 : 513.49
MDL号 : MFCD08669741
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(204.48 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Caspase-3

    Caspase-3, IC50:25 nM-400 nM

  • Caspase-8

    Caspase-8, IC50:25 nM-400 nM

  • Caspase-9

    Caspase-9, IC50:25 nM-400 nM

  • Caspase-1

    Caspase-1, IC50:25 nM-400 nM
描述 Apoptosis is mediated by specific initiating and effector cysteine proteases (caspases) that are unique in cleaving substrates specifically following aspartate residues. The activation of specific caspases has defined three major pathways that can carry out the apoptotic process[6]. Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties, and it inhibits caspase 7 with IC50 of 48 nM and 25 - 400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12[7]. The broad spectrum caspase inhibitor, Boc-D-fmk, completely prevents apoptosis in WEHI 231 cells at 50 µM, but is ineffective at lower doses. In striking contrast, the caspase inhibitor Q-VD-OPh dramatically prevents DNA fragmentation at concentrations as low as 5 µM[6]. Analysis of 5 µM Q-VD-OPh in the presence of actinomycin D in WEHI 231 cells for at least 48 h results in no change in the cell number and complete cellular viability as determined by cell number and trypan blue exclusion[6]. Similar to WEHI 231 cells, the presence of 5 µM Q-VD-OPh completely prevents the actinomycin D-induced DNA fragmentation and apoptosis from occurring in Jurkat T cells[6]. TGF beta induced apoptosis in HRP-1 cells within 24 h, as determined by DNA laddering, and this is completely inhibited by 5 µM Q-VD-OPh, consistent with other cell lines[6]. C57BL/6 mice with ischemic ARF treated with Q-VD-OPh has a marked (100%) reduction in blood urea nitrogen (BUN) and serum creatinine and a highly significant reduction in morphological acute tubular necrosis (ATN) score compared with vehicle-treated mice[8]. Two-day-old Swiss-Webster mice are infected with 104 PFU of myocarditic virus, followed by the administration of Q-VD-Oph, Z-VAD(OMe)-FMK, or their diluent controls on days 3 to 6 postinfection. Mice receiving caspase inhibitors shows statistically significant reductions in myocardial injury scores compared to controls, as measured by two independent myocardial injury scoring systems[9].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.19mL

9.74mL

1.95mL

0.97mL

19.47mL

3.89mL

1.95mL
参考文献

[1]Caserta TM, Smith AN, et al. Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties. Apoptosis. 2003 Aug;8(4):345-52

[2]Caserta TM, Smith AN, et al. Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties. Apoptosis. 2003 Aug;8(4):345-52.

[3]Sanders EJ, Parker E, et al. Retinal ganglion cell survival in development: mechanisms of retinal growth hormone action. Exp Eye Res. 2006 Nov;83(5):1205-14. Epub 2006 Aug 7.

[4]Colak A, Antar V, et al. Q-VD-OPh, a pancaspase inhibitor, reduces trauma-induced apoptosis and improves the recovery of hind-limb function in rats after spinal cord injury. Neurocirugia (Astur). 2009 Dec;20(6):533-40; discussion 540.

[5]Renolleau S, Fau S, et al. Specific caspase inhibitor Q-VD-OPh prevents neonatal stroke in P7 rat: a role for gender. J Neurochem. 2007 Feb;100(4):1062-71. Epub 2006 Dec 12.

[6]Caserta TM, Smith AN, Gultice AD, Reedy MA, Brown TL. Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties. Apoptosis. 2003 Aug;8(4):345-52. doi: 10.1023/a:1024116916932. PMID: 12815277.

[7]Rohn TT, Kokoulina P, Eaton CR, Poon WW. 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. PMID: 20057974; PMCID: PMC2802048.

[8]Melnikov VY, Faubel S, Siegmund B, Lucia MS, Ljubanovic D, Edelstein CL. Neutrophil-independent mechanisms of caspase-1- and IL-18-mediated ischemic acute tubular necrosis in mice. J Clin Invest. 2002 Oct;110(8):1083-91. doi: 10.1172/JCI15623. PMID: 12393844; PMCID: PMC150794.

[9]DeBiasi RL, Robinson BA, Sherry B, Bouchard R, Brown RD, Rizeq M, Long C, Tyler KL. Caspase inhibition protects against reovirus-induced myocardial injury in vitro and in vivo. J Virol. 2004 Oct;78(20):11040-50. doi: 10.1128/JVI.78.20.11040-11050.2004. PMID: 15452224; PMCID: PMC521817.