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Z-IETD-FMK Z-IE(OMeTD(OMe)-FMK)

Z-IETD-FMK (Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK)是一种特异性Caspase-8抑制剂。Z-IETD-FMK也是颗粒酶B(granzyme B)抑制剂。

  • 货号:
    TK0162
  • 规格:
    1mg
  • 价格:
    0.00

产品参数

CAS No.210344-98-2
生物活性Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
分子式C30H43FN4O11
分子量654.68
运输条件Room temperature in continental US; may vary elsewhere.
储存条件Powder -20℃ 3 years
溶解性数据DMSO : 41.67 mg/mL (63.65 mM; Need ultrasonic)
体内研究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.
体外研究Z-IETD-FMK causes full inhibition only of the proapoptotic effect of TNFα with an IC50 of 0.46 μM. 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. 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.
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