Z-IETD-AFC, a specific fluorescence substrate, can be used to determine the caspase-8 catalytic activity[1].
分子量
821.75
Formula
C37H42F3N5O13
CAS 号
219138-02-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Boudard D, et al. Increased caspase-3 activity in refractory anemias: lack of evidence for Fas pathway implication. Leukemia. 2002;16(11):2343-2345.
Z-IETD-AFC, a specific fluorescence substrate, can be used to determine the caspase-8 catalytic activity[1].
分子量
821.75
Formula
C37H42F3N5O13
CAS 号
219138-02-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Boudard D, et al. Increased caspase-3 activity in refractory anemias: lack of evidence for Fas pathway implication. Leukemia. 2002;16(11):2343-2345.
Z-IETD-AFC, a specific fluorescence substrate, can be used to determine the caspase-8 catalytic activity[1].
分子量
821.75
Formula
C37H42F3N5O13
CAS 号
219138-02-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Boudard D, et al. Increased caspase-3 activity in refractory anemias: lack of evidence for Fas pathway implication. Leukemia. 2002;16(11):2343-2345.
This 14-mer prosaptide sequence is derived from the active neurotrophic region in the amino-terminal portion of the saposin C domain. Synthetic peptides derived from this region are biologically active and are named ?prosaptides.? Prosaposin and prosaptides are active on a variety of neuronal cells, stimulating sulfatide synthesis and increasing sulfatide concentration in Schwann cells and oligodendrocytes. This indicates that prosaposin and prosaptides are trophic factors for myelin formation.
溶解度
分子量
1515.6
化学式
C74H86N10O25
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) 是一种具有细胞渗透作用的选择性 caspase-8 抑制剂。Z-IETD-FMK 也是颗粒酶 B (granzyme B) 抑制剂。
Z-IETD-FMK Chemical Structure
CAS No. : 210344-98-2
规格
价格
是否有货
数量
10 mM * 1 mL in DMSO
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1 mg
¥1400
In-stock
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¥3000
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10 mg
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50 mg
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Z-IETD-FMK 相关产品
•相关化合物库:
Bioactive Compound Library Plus
Peptidomimetic Library
Peptide Library
生物活性
Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor[1]. Z-IETD-FMK is also a granzyme B inhibitor[5].
IC50 & Target[1]
Caspase-8
体外研究 (In Vitro)
Z-IETD-FMK causes full inhibition only of the proapoptotic effect of TNFα with an IC50 of 0.46 μM[1]. Z-IETD-FMK and Z-VAD-FMK at non-toxic doses are found to be immunosuppressive and inhibit human T cell proliferation induced by mitogens and IL-2. They are shown to block NF-κB in activated primary T cells, but have little inhibitory effect on the secretion of IL-2 and IFN-γ during T cell activation[2]. Z-IETD-FMK inhibits the cleavage of caspase-8 and only partially inhibits the cleavage of caspase-3 and PARP. Z-IETD-FMK can prevent the execution of apoptosis in retinal cells exposed to different apoptotic stimuli[3].
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)
Pharmacological inhibition of caspase-8 by z-IETD-FMK robustly reduces tumour outgrowth and this is closely associated with a reduction in the release of pro-inflammatory cytokines, IL-6, TNF-α, IL-18, IL-1α, IL-33, but not IL-1β. Furthermore, inhibition of caspase-8 reduces the recruitment of innate suppressive cells, such as myeloid-derived suppressor cells, but not of regulatory T cells to lungs of tumour-bearing mice[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.
分子量
654.68
Formula
C30H43FN4O11
CAS 号
210344-98-2
Sequence
Z-Ile-Glu-Thr-Asp-FMK
Sequence Shortening
ZIETDFMK
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Cowburn AS, et al. z-VAD-fmk augmentation of TNF alpha-stimulated neutrophil apoptosis is compound specific and does not involve the generation of reactive oxygen species.
[2]. Lawrence CP, et al. 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.
[3]. Tezel G, et al. Inhibition of caspase activity in retinal cell apoptosis induced by various stimuli in vitro. Invest Ophthalmol Vis Sci. 1999 Oct;40(11):2660-7.
[4]. Terlizzi M, et al. Pharmacological inhibition of caspase-8 limits lung tumour outgrowth. Br J Pharmacol. 2015 Aug;172(15):3917-28.
[5]. Yang J, et al. Granzyme B Is an Essential Mediator in CD8+ T Cell Killing of Theileria parva-Infected Cells.Infect Immun. 2018 Dec 19;87(1). pii: e00386-18.
Cell Assay [2]
T cell proliferation following mitogen stimulation is determined using [3H]-thymidine incorporation. In brief, PBMCs or purified T cells are seeded at 1×106 cells/mL in 96 well plates and stimulated with either PHA (5 μg/mL or co-stimulated with anti-CD3 mAb (5 μg/mL) and anti-CD28 mAb (2.5 μg/mL) in the presence or absence of caspase inhibitor Z-IETD-FMK. The cells are cultured for 72 h with the last 16 h pulsed with [[3H]-labelled methyl-thymidine (0.037 MBq) prior to harvest onto glass fibre filter mats using a Tomtec automated multi-well harvester[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.
Animal Administration [4]
Mice: Mice are divided into three groups: (1) naive, non-treated, mice; (2) CTR (control), i.t. instilled with NMU; and (3) lung cancer-bearing mice treated with Z-IETD-FMK (0.5 μg per mouse). The involvement of caspase-8 in lung cancer development is the determined at different time points (3, 7 and 28 days)[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.
参考文献
[1]. Cowburn AS, et al. z-VAD-fmk augmentation of TNF alpha-stimulated neutrophil apoptosis is compound specific and does not involve the generation of reactive oxygen species.
[2]. Lawrence CP, et al. 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.
[3]. Tezel G, et al. Inhibition of caspase activity in retinal cell apoptosis induced by various stimuli in vitro. Invest Ophthalmol Vis Sci. 1999 Oct;40(11):2660-7.
[4]. Terlizzi M, et al. Pharmacological inhibition of caspase-8 limits lung tumour outgrowth. Br J Pharmacol. 2015 Aug;172(15):3917-28.
[5]. Yang J, et al. Granzyme B Is an Essential Mediator in CD8+ T Cell Killing of Theileria parva-Infected Cells.Infect Immun. 2018 Dec 19;87(1). pii: e00386-18.
This biotinylated apopain inhibitor has successfully been used for the affinity purification, on a streptavidin-agarose column, of caspase-3 (apopain); the enzyme that cleaves the poly(ADP-ribose) polymerase (PARP). This inhibitor showed an inhibitory act
溶解度
分子量
502.5
化学式
C21H34N4O10
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
Z. Han et al, J. Biol Chem., 272, 13422 (1997) M.Garcia-Calvo et al., J. Biol. Chem., 273, 32608 (1998)