Q-VD(OMe)-OPh
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Q-VD-OPh（quinolyl-valyl-O-methylaspartyl-[-2,6-di?uorophenoxy]-methyl ketone）是一种广谱的caspase抑制剂，提供了一种低成本的、无毒的和高特异性的凋亡抑制方式，并为新抑制剂的设计提供了全新的视角[1]。与广泛使用的抑制剂ZVAD-fmk和Boc-D-fmk相比，Q-VD-OPh更有效地抑制细胞凋亡。Q-VD-OPh同等有效地抑制三大凋亡途径caspase 9/3、caspase 8/10和caspase 12介导的细胞凋亡。Q-VD-OPh可以抑制重组的caspases 1、3、8和9，IC50值介于25-400 nM之间。除了效力的增加，Q-VD-OPh对细胞是无毒的，即使在高浓度下。Q-VD-OPh在不到4小时的时间内完全抑制凋亡诱导子诱导的大量细胞死亡，证实了Q-VD-OPh作为凋亡抑制剂的效力[2]。Q-VD-OPh抑制放线菌素D（actinomycin D）诱导的大量细胞凋亡。
参考文献：
1. T. M. Caserta, A. N. Smith, A. D. Gultice, M. A. Reedy and T. L. Brown, Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties, Apoptosis 2003; 8: 345–352
2. Yin XM. Signal transduction mediated by Bid, a pro-death Bcl-2 family proteins, connects the death receptor and mitochondria apoptosis pathways. Cell Res 2000; 10: 161–167
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- 6. PIUS REYDERG AGYEMANG. "Profifiling of FDA-Approved and Clinical Trial Drugs Revealed Shared Cytotoxicity And Collateral Sensitivity In Resistant (H69ar) And Non-Resistant (H69) Small Cell Lung Cancer Cells. (Drug Repurposing in Cancer Chemotherapy)." South Dakota State University 2021.
- 7. Martens AWJ, Janssen SR, et al. "CD3xCD19 DART molecule treatment induces non-apoptotic killing and is efficient against high-risk chemotherapy and venetoclax-resistant chronic lymphocytic leukemia cells." J Immunother Cancer. 2020;8(1):e000218. PMID: 32581054
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- 9. Robeson AC, Lindblom KR, et al. "Dimer-specific immunoprecipitation of active caspase-2 identifies TRAF proteins as novel activators." EMBO J. 2018 Jun 6. pii: e97072. PMID: 29875129
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 527 |
| Formula | C26H25F2N3O6 |
| Synonyms | Q-VD(OMe)-OPh |
| Solubility | ≥26.35 mg/mL in DMSO; insoluble in H2O; ≥97.4 mg/mL in EtOH |
| Chemical Name | (S)-methyl 5-(2,6-difluorophenoxy)-3-((S)-3-methyl-2-(quinoline-2-carboxamido)butanamido)-4-oxopentanoate |
| SDF | Download SDF |
| Canonical SMILES | O=C(N[C@@H](C(C)C)C(N[C@@H](CC(OC)=O)C(COC1=C(F)C=CC=C1F)=O)=O)C2=NC3=CC=CC=C3C=C2 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验: [1] | |
|
细胞系 |
小鼠未成熟B细胞WEHI 231未成熟细胞系 |
|
制备方法 |
该化合物在DMSO中的溶解度大于10 mM，若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月 |
|
反应条件 |
4 h，50 μg/mL |
|
实验结果 |
为了分析广谱caspase抑制剂对WEHI 231细胞中放线菌素D诱导的凋亡的影响，在4小时后分析DNA片段化，当没有caspase抑制剂存在时，细胞发生实质性细胞凋亡。在1 μg/ml放线菌素D存在下，使用剂量减少的Q-VD-OPh孵育，结果表明该化合物以剂量依赖性方式抑制凋亡。 |
| 动物实验: [2] | |
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动物模型 |
P7大鼠 |
|
给药剂量 |
1 mg/kg，腹腔注射 |
|
实验结果 |
Q-VD-OPh减轻新生儿中风后的脑损伤。将P7大鼠进行左中脑动脉电凝和瞬时同侧颈总动脉闭塞50分钟，然后恢复48小时。与对照缺血动物相比（12.6 ± 2.8，n = 16，p = 0.006），单次注射Q-VD-OPh显著减少了48％的梗塞体积，没有大鼠死亡。与对照组动物相比，Q-VD-OPh还诱导TUNEL阳性细胞数目的明显减少。 |
|
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
References: [1] Caserta T M, Smith A N, Gultice A D, et al. Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties[J]. Apoptosis, 2003, 8(4): 345-352. [2] Renolleau S, Fau S, Goyenvalle C, et al. Specific caspase inhibitor Q‐VD‐OPh prevents neonatal stroke in P7 rat: a role for gender[J]. Journal of neurochemistry, 2007, 100(4): 1062-1071. |
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| 描述 | Q-VD(OMe)-Oph是caspase的抑制剂。 | |||||
| 靶点 | Caspase | |||||
| IC50 | ||||||
质量控制和MSDS
- 批次:
化学结构
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