小分子抑制剂

Small molecule inhibitor

Z-IETD-FMK

货号:HY-101297
规格:
名称:Synonyms: Z-IE(OMe)TD(OMe)-FMK

产品详情

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
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 -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°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

     

     
  • 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

     

     
  • 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

     

     
*以上所有助溶剂都可在 MCE 网站选购。
参考文献