Biotin-VAD-FMK is a cell permeable, irreversible biotin-labeled caspase inhibitor, used to identify active caspases in cell lysates.
IC50 & Target
Caspase
体外研究 (In Vitro)
Biotin-VAD-FMK is a synthetic peptide designed as a methyl ester to facilitate cell permeability.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
To examine whether caspase-2 is activated in the absence of proteolytic cleavage, an in vivo affinity labeling approach is used, using the biotinylated caspase inhibitor biotin-VAD-fmk that detects only active caspases[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
672.81
Formula
C30H49FN6O8S
CAS 号
1135688-15-1
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Li J, et al. Nitric oxide suppresses apoptosis via interrupting caspase activation and mitochondrial dysfunction in cultured hepatocytes. J Biol Chem. 1999 Jun 11;274(24):17325-33.
[2]. Samraj AK, et al. Loss of caspase-9 reveals its essential role for caspase-2 activation and mitochondrial membranedepolarization. Mol Biol Cell. 2007 Jan;18(1):84-93.
Z-VAD-FMK (Z-VAD(OH)-FMK) 是一种 pan caspase 抑制剂。Z-VAD-FMK 不抑制泛素 C 末端水解酶 L1 (UCHL1) 活性,即使浓度高达 440 μM。
Z-VAD-FMK Chemical Structure
CAS No. : 161401-82-7
规格
价格
是否有货
数量
10 mM * 1 mL in DMSO
¥3090
In-stock
1 mg
¥875
In-stock
5 mg
¥3085
In-stock
10 mg
¥5270
In-stock
50 mg
询价
100 mg
询价
* Please select Quantity before adding items.
Z-VAD-FMK 相关产品
•相关化合物库:
Covalent Screening Library Plus
Bioactive Compound Library Plus
Apoptosis Compound Library
Anti-Cancer Compound Library
Covalent Screening Library
生物活性
Z-VAD-FMK (Z-VAD(OH)-FMK) is a well-know pan caspase inhibitor, which does not inhibit ubiquitin carboxy-terminal hydrolase L1 (UCHL1) activity even at concentrations as high as 440 μM[1].
IC50 & Target[1]
Caspase
体外研究 (In Vitro)
Z-VAD-FMK (40 μM) reverses the apoptotic effect exerted by total saponin of Solanum lyratum Thunb (TSSLT) in Hela cells. HeLa cells are pretreated with Z-VAD-FMK (40 μM) for 30 min and exposed to TSSLT (6 μg/mL) for 48 h[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
Cell Line:
HeLa cells
Concentration:
40 μM
Incubation Time:
Prtreated for 30 minutes
Result:
Prevented TSSLT-induced cell death. More than 80% cell survival was observed.
分子量
453.46
Formula
C21H28FN3O7
CAS 号
161401-82-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:
DMSO : 100 mg/mL (220.53 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
2.2053 mL
11.0263 mL
22.0527 mL
5 mM
0.4411 mL
2.2053 mL
4.4105 mL
10 mM
0.2205 mL
1.1026 mL
2.2053 mL
*
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 (sealed storage, away from moisture and light)。-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:
[1]. Davies CW, et al. The co-crystal structure of ubiquitin carboxy-terminal hydrolase L1 (UCHL1) with a tripeptide fluoromethyl ketone (Z-VAE(OMe)-FMK). Bioorg Med Chem Lett. 2012 Jun 15;22(12):3900-4.
[2]. Liu HR, et al. Antiproliferative activity of the total saponin of Solanum lyratum Thunb in Hela cells by inducing apoptosis. Pharmazie. 2008 Nov;63(11):836-42.
Z-VAD(OMe)-FMK (Z-Val-Ala-Asp(OMe)-FMK) is a cell-permeable and irreversible pan-caspase inhibitor[1]. Z-VAD(OMe)-FMK is an ubiquitin carboxy-terminal hydrolase L1 (UCHL1) inhibitor. Z-VAD(OMe)-FMK irreversibly modifies UCHL1 by targeting the active site of UCHL1[2].
IC50 & Target[1]
Caspase
体外研究 (In Vitro)
Z-VAD(OMe)-FMK (Z-Val-Ala-Asp(OMe)-FMK) is a broad-spectrum caspase inhibitor, has been shown to inhibit the intracellular activation of caspase-like proteases. The injection of Z-VAD(OMe)-FMK suppresses the caspase-3 activity in lung tissues, and significantly decreases the number of terminal dUTP nick-end labeling-positive cells[1]. Z-VAD(OMe)-FMK effectively inhibits UCHL1’s reaction with hemagglutinin-tagged ubiquitin vinylmethyl ester (HA-UbVME) at the concentration of 100 μM[2]. Z-VAD(OMe)-FMK is administered intraperitoneally at 1 hour before and 6 hours after SAH. Expression of caspase-3 and positive TUNEL is examined as markers for apoptosis. Z-VAD(OMe)-FMK suppresses TUNEL and caspase-3 staining in endothelial cells, decreases caspase-3 activation, reduces BBB permeability, relieves vasospasm, abolishes brain edema, and improves neurological outcome[3]. Z-VAD(OMe)-FMK is a cell-permeable caspase inhibitor, efficiently blocks cell death induced by SMN deficiency[4].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
The survival rate of mice is prolonged significantly by the injection of Z-VAD(OMe)-FMK (Z-Val-Ala-Asp(OMe)-FMK). All mice succumbed to LPS within 30 hours. By contrast, the mice treated with Z-VAD(OMe)-FMK survive significantly longer and 27% of the mice survived more than 7 days[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
467.49
Formula
C22H30FN3O7
CAS 号
187389-52-2
Sequence
Z-Val-Ala-Asp(OMe)-FMK
Sequence Shortening
ZVA-D(OMe)-FMK
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Kawasaki M, et al. Protection from lethal apoptosis in lipopolysaccharide-induced acute lung injury in mice by a caspaseinhibitor. Am J Pathol. 2000 Aug;157(2):597-603.
[2]. Davies CW, et al. The co-crystal structure of ubiquitin carboxy-terminal hydrolase L1 (UCHL1) with a tripeptide fluoromethyl ketone (Z-VAE(OMe)-FMK). Bioorg Med Chem Lett. 2012 Jun 15;22(12):3900-4.
[3]. Park S, et al. Neurovascular protection reduces early brain injury after subarachnoid hemorrhage. Stroke. 2004 Oct;35(10):2412-7.
[4]. Ilangovan R, et al. Inhibition of apoptosis by Z-VAD-fmk in SMN-depleted S2 cells. J Biol Chem. 2003 Aug 15;278(33):30993-9.
Cell Assay [4]
PCR products containing coding sequences for the dSMN (forward primer: 5′-TAA TAC GAC TCA CTA TAG GG AAG ACG TAC GAC GAG TCG-3′; and reverse primer: 5′-TAA TAC GAC TCA CTA TAG GG GTG GTG CTG GCT TCT TTC-3′; product length, 601bps; bold and italics letters represent T7 promoter sequences) and control Drosophila Presenilin (dPsn) gene (forward primer: 5′-TAA TAC GAC TCA CTA TAG GG TG GCT GCT GTC AAT CTC-3′; and reverse primer: 5′-TAA TAC GAC TCA CTA TAG GG CGA TAG CAA CGC TTC TTG-3′; product length: 543bps) are obtained and gel-purified. Double-stranded RNAs (dsRNA) are generated by transcription with Ribomax T7 Transcription kit and digested with Rnase-free DNase. The dsRNA products are ethanol precipitated and annealed by incubation at 65°C for 30 min and then slowly allowed to cool at room temperature. The annealed dsRNA products are analyzed on a 1% agaorse gel to ensure the majority of dsRNA existed as a single band. The dsRNA (2 μg) and/or plasmid DNAs (2 μg) are introduced into cells by using Cellfectin. Caspase inhibition is achieved by using 50 μM of Z-VAD(OMe)-FMK in the culture medium[4].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [1][3]
Mice[1] Mice used in this study are 5- to 6-week-old (20 to 22 g) ICR males. Mice are injected with 30 mg/kg LPS from E. coli serotype O111:B4 through the tail vein. A single intravenous injection of Z-VAD(OMe)-FMK (0.25 mg) is made 15 minutes before LPS injection, followed by three intravenous injections of Z-VAD(OMe)-FMK (0.1 mg each) per hour. Control mice are injected with the same volume of 1% DMSO in sterile saline. Rats[3] Male Sprague-Dawley rats weighing 300 to 350 g are anesthetized with α-chloralose (40 mg/kg IP) and urethane (400 mg/kg IP). Animals are intubated, and respiration is maintained with a small animal respirator. Rectal temperature is maintained at 37±0.5°C with a heating pad. The left external carotid artery is isolated and a 4.0 monofilament nylon suture is inserted through the internal carotid artery to perforate the middle cerebral artery. SAH is confirmed at autopsy in each rat. Sham-operated rats underwent the same procedures except that the suture is withdrawn after resistance is felt. Z-VAD(OMe)-FMK (50 μM per 0.3 mL) is injected intraperitoneally at 1 hour before and 6 hours after SAH induction. In vehicle group, rats underwent SAH induction and are treated with the same volume of vehicle (DMSO diluted in physiological buffer solution). No treatment is applied in sham-operated animals.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Kawasaki M, et al. Protection from lethal apoptosis in lipopolysaccharide-induced acute lung injury in mice by a caspaseinhibitor. Am J Pathol. 2000 Aug;157(2):597-603.
[2]. Davies CW, et al. The co-crystal structure of ubiquitin carboxy-terminal hydrolase L1 (UCHL1) with a tripeptide fluoromethyl ketone (Z-VAE(OMe)-FMK). Bioorg Med Chem Lett. 2012 Jun 15;22(12):3900-4.
[3]. Park S, et al. Neurovascular protection reduces early brain injury after subarachnoid hemorrhage. Stroke. 2004 Oct;35(10):2412-7.
[4]. Ilangovan R, et al. Inhibition of apoptosis by Z-VAD-fmk in SMN-depleted S2 cells. J Biol Chem. 2003 Aug 15;278(33):30993-9.