Ac-IETD-AMC

Ac-IETD-AMC;

Ac-IETD-AMC 是一种含有乙酰基 (Ac) 部分的荧光 caspase-8/颗粒酶 B 底物。Ac-IETD-AMC 经常用于测量 caspase-8 活性。

Ac-IETD-AMCamp;;

Ac-IETD-AMC Chemical Structure

CAS No. : 348079-17-4

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生物活性

Ac-IETD-AMC is a fluorogenic caspase-8/granzyme B substrate containing the acetyl (Ac) moiety. Ac-IETD-AMC is frequently used to measure caspase-8 activity[1].

分子量

675.68

Formula

C31H41N5O12

CAS 号

348079-17-4

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]. V Frost, et al. Exploitation of a non-apoptotic caspase to regulate the abundance of the cdkI p27(KIP1) in transformed lymphoid cells. Oncogene. 2001 May 17;20(22):2737-48.

Ac-IETD-AFC

Ac-IETD-AFC;

Ac-IETD-AFC 是 caspase-8、caspase-3、caspase-10 和颗粒酶 B 的荧光底物。

Ac-IETD-AFCamp;;

Ac-IETD-AFC Chemical Structure

CAS No. : 211990-57-7

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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生物活性

Ac-IETD-AFC is a fluorogenic substrate of caspase-8, caspase-3, caspase-10, and granzyme B[1].

分子量

729.65

Formula

C31H38F3N5O12

CAS 号

211990-57-7

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]. [1]Kazimierz Weglarczyk, et al. Caspase-8 activation precedes alterations of mitochondrial membrane potential during monocyte apoptosis induced by phagocytosis and killing of Staphylococcus aureus. Infect Immun. 2004 May;72(5):2590-7.

    [2]. Przemysław Reszka, et al. Synthesis, enzymatic evaluation, and docking studies of fluorogenic caspase 8 tetrapeptide substrates. ChemMedChem. 2010 Jan;5(1):103-17.

Z-IETD-AFC

Z-IETD-AFC;

Z-IETD-AFC 是一种特异的荧光底物,可用于测定 caspase-8 的催化活性。

Z-IETD-AFCamp;;

Z-IETD-AFC Chemical Structure

CAS No. : 219138-02-0

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
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生物活性

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-FMK(Synonyms: Z-IE(OMe)TD(OMe)-FMK)

Z-IETD-FMK;(Synonyms: Z-IE(OMe)TD(OMe)-FMK) 纯度: ge;98.0%

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-FMKamp;;(Synonyms: Z-IE(OMe)TD(OMe)-FMK)

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 ¥4321 In-stock
1 mg ¥1400 In-stock
5 mg ¥3000 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

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Z-IETD-FMK 相关产品

bull;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].

MCE 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].

MCE 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.

储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : 41.67 mg/mL (63.65 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5275 mL 7.6373 mL 15.2746 mL
5 mM 0.3055 mL 1.5275 mL 3.0549 mL
10 mM 0.1527 mL 0.7637 mL 1.5275 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。-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:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂:;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.08 mg/mL (3.18 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.18 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂:;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.18 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.18 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂:;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.18 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.18 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
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.

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].

MCE 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].

MCE 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.