>>Signaling Pathways>> Apoptosis>> Caspase>>Z-VAD-FMK

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.

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Z-VAD-FMK Chemical Structure

Cas No.: 187389-52-2

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$103.00
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1mg
US$40.00
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5mg
US$109.00
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10mg
US$195.00
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25mg
US$274.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 13 publications

Product Documents

Quality Control & SDS

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Protocol

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.

Background

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.

Chemical Properties

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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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    Z-VAD-FMK- GlpBio

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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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