Z-VAD-FMK (Synonyms: Benzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone,Z-Val-Ala-Asp(OMe)-FMK) |
Catalog No.GC12861 |
Z-VAD-FMK (Z-Val-Ala-Asp(OMe)-FMK)는 세포막 침투성이 있고 불가역적인 팬카스패이스 억제제입니다. Z-VAD-FMK는 유비퀴틴 카르복시 터미널 하이드롤레이즈 L1 (UCHL1) 억제제입니다. Z-VAD-FMK는 UCHL1의 활성부위를 대상으로하여 UCHL1을 불가역적으로 수정합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 187389-52-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
CD4+ and CD8+ T cells |
Preparation Method |
Soluble in DMSO to 20 mM |
Reaction Conditions |
100 μM, 24 h |
Applications |
Z-VAD-FMK is immunosuppressive in vitro and inhibit T cell proliferation without blocking the processing of caspase-8 and caspase-3. |
Animal experiment [2]: | |
Animal models |
C57BL/6 Mice (Treatment with LPS) |
Preparation Method |
Soluble in DMSO to 20 mM |
Dosage form |
20 μg/g, i.p. |
Applications |
Z-VAD-FMK treatment alleviates LPS-induced endotoxic shock by inducing macrophage necroptosis and promoting MDSC-mediated inhibition of macrophage activation. |
References: [1]. Lawrence CP, Chow SC. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties. Toxicol Appl Pharmacol. 2012 Nov 15;265(1):103-12. [2]. Li X, Yao X, Zhu Y, et al. The Caspase Inhibitor Z-VAD-FMK Alleviates Endotoxic Shock via Inducing Macrophages Necroptosis and Promoting MDSCs-Mediated Inhibition of Macrophages Activation. Front Immunol. 2019 Aug 2;10:1824. |
Z-VAD-FMK (벤질옥시카보닐-발-알라-아스파르트산 (OMe) 플루오로메틸케톤)은 ICE와 유사한 프로테아제 억제제로, CPP32의 활성형태 형성을 방지하여 세포 사멸을 억제합니다. [3]
Z-VAD-FMK는 체외에서 면역억제 작용을 가지며, 카스패이스-8 및 카스패이스-3의 처리를 차단하지 않으면서 T 세포 증식을 억제합니다. Z-VAD-FMK는 anti-CD3 및 anti-CD28 또는 PHA에 의해 유도된 T 세포 증식을 억제할 수 있습니다. 또한 z-VAD-FMK는 아포토시스 중 카스패이스 처리를 억제하지만 T 세포 활성화 중에는 그렇지 않습니다. Z-VAD-FMK는 체외에서 종양세포의 카스패이스 처리와 아포토시스 유도를 억제합니다 (IC50=0.0015 - 5.8 mM). [1]
Z-VAD-FMK는 특정 자극 하에서 네크로프토시스를 유도하는 데 사용될 수 있습니다. Z-VAD-FMK로 마우스를 치료하면, 리폴리사카라이드(LPS) 도전 후 사망률을 크게 감소시키고 질병을 완화할 수 있습니다. 특히 LPS 도전된 마우스에서 Z-VAD-FMK 처리는 네크로 프트 시스를 촉진하여 복막 거대세포의 비율을 줄이고 거대 세포의 염증 반응을 억제함으로써 작용합니다. 게다가 Z-VAD-FMK 예처리는 골수 유래 거대 세포(BMDM)의 LPS 유도 일산화질소 매개 네크로 프트 시스를 촉진하여 염증성 사이토킷인 분비량을 감소시켜줍니다. 재미있게도, Z-VAD-FMK 처리는 내독 소격자 모델에서골수 유래 억제 세포(MDSCs) 축적을 촉진하며 이 과정은 거대 세포의 LPS 유발 염증 반응 억제에 기여합니다. 따라서, Z-VAD-FMK 처리는 거대 세포 네크로 프트 시스를 유도하고 MDSC 매개의 거대 세포 활성 억제를 촉진하여 LPS 유발 내독 소격자를 완화시킵니다. 생체 내 실험에서, 마우스는 Z-VAD-FMK(5, 10 및 20 μg/g 체중) 또는 차량(생리식염수)으로 2시간 동안 예처리 또는 후처리되며, 내복 주사로 LPS(10 μg/g 체중)가 유도되고 대조군으로 생리식염수가 사용됩니다. [2]
References:
[1]. Lawrence CP, Chow SC. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties. Toxicol Appl Pharmacol. 2012 Nov 15;265(1):103-12.
[2]. Li X, Yao X, Zhu Y, et al. The Caspase Inhibitor Z-VAD-FMK Alleviates Endotoxic Shock via Inducing Macrophages Necroptosis and Promoting MDSCs-Mediated Inhibition of Macrophages Activation. Front Immunol. 2019 Aug 2;10:1824.
[3]. Slee EA, Zhu H, et al. Benzyloxycarbonyl-Val-Ala-Asp (OMe) fluoromethylketone (Z-VAD.FMK) inhibits apoptosis by blocking the processing of CPP32. Biochem J. 1996 Apr 1;315 (Pt 1) (Pt 1):21-4.
Cas No. | 187389-52-2 | SDF | |
Synonyms | Benzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone,Z-Val-Ala-Asp(OMe)-FMK | ||
Chemical Name | methyl (3S)-5-fluoro-3-[[(2S)-2-[[(2S)-3-methyl-2-(phenylmethoxycarbonylamino)butanoyl]amino]propanoyl]amino]-4-oxopentanoate | ||
Canonical SMILES | CC(C)C(C(=O)NC(C)C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)OCC1=CC=CC=C1 | ||
Formula | C22H30FN3O7 | M.Wt | 467.49 |
Solubility | ≥ 23.37mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.1391 mL | 10.6954 mL | 21.3908 mL |
5 mM | 0.4278 mL | 2.1391 mL | 4.2782 mL |
10 mM | 0.2139 mL | 1.0695 mL | 2.1391 mL |
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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