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.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

513.49

C₂₆H₂₅F₂N₃O₆

1135695-98-5

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 100 mg/mL (194.75 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (4.05 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.05 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.08 mg/mL (4.05 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.05 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (4.05 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.05 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.

  [5]. Laforge M, et al. The anti-caspase inhibitor Q-VD-OPH prevents AIDS disease progression in SIV-infected rhesus macaques. J Clin Invest. 2018 Apr 2;128(4):1627-1640.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.

  [5]. Laforge M, et al. The anti-caspase inhibitor Q-VD-OPH prevents AIDS disease progression in SIV-infected rhesus macaques. J Clin Invest. 2018 Apr 2;128(4):1627-1640.