Z-IETD-FMK

製品コードS7314 バッチS731403

印刷

化学情報

 Chemical Structure Synonyms Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C30H43FN4O11

分子量 654.68 CAS No. 210344-98-2
Solubility (25°C)* 体外 DMSO 100 mg/mL (152.74 mM)
Water Insoluble
Ethanol Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

5.000mg/ml (7.64mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Z-IETD-FMK (Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK) is a specific Caspase-8 inhibitor. Z-IETD-FMK is also an inhibitor of granzyme B.
in vitro

Z-IETD-FMK, which inhibits the cleavage of caspase-8 and partially inhibits the cleavage of caspase-3 and PARP, prevents the execution of apoptosis in retinal cells exposed to different apoptotic stimuli. [1]

This compound (50 μM) reduces ceramide-induced cardiomyocyte death and significantly inhibits the activation of caspase 3. [2]

Inhibition of caspase-8 by this chemical affects the generation of activated/memory T cells and T cell cytokine production, and decreases NF-kappaB responses to TCR:CD3 engagement in T cell cultures. [3]

in vivo

In vivo, inhibition of caspase-8 by Z-IETD-FMK reduces memory/activated CD4 and CD8 T cells, and increases susceptibility to T. cruzi infection. [3]

This compound promotes neuronal survival and regeneration of injured retinal ganglion cells after CNS injuries. [4]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Rat neonatal cardiomyocytes
濃度 50 µM
反応時間 24 h
実験の流れ

Drugs were added to the cell culture medium simultaneously with ceramide, and surviving cells were counted 24 hours later.

動物実験 動物モデル T. cruzi-infected mice
投薬量 0.4 mg/3 days
投与方法 --

参考

  • https://pubmed.ncbi.nlm.nih.gov/10509663/
  • https://pubmed.ncbi.nlm.nih.gov/10997751/
  • https://pubmed.ncbi.nlm.nih.gov/15879131/
  • https://pubmed.ncbi.nlm.nih.gov/21775595/

カスタマーフィードバック

Data from [Data independently produced by , , Cell Physiol Biochem, 2017, 42(5):1822-1836]

Data from [Data independently produced by , , Int J Oncol, 2018, 52(3):1023-1032]

Data from [Data independently produced by , , Drug Des Devel Ther, 2017, 11:2841-2850]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

GZMK-expressing CD8+ T cells promote recurrent airway inflammatory diseases [ Nature, 2025, 10.1038/s41586-024-08395-9] PubMed: 39814882
The intrinsic expression of NLRP3 in Th17 cells promotes their protumor activity and conversion into Tregs [ Cell Mol Immunol, 2025, 22(5):541-556] PubMed: 40195474
Homologous recombination promotes non-immunogenic mitotic cell death upon DNA damage [ Nat Cell Biol, 2025, 27(1):59-72] PubMed: 39805921
PI3K/AKT signaling mediates stress-inducible amyloid formation through c-Myc [ Cell Rep, 2025, 44(5):115617] PubMed: 40272983
Eimeria tenella AMA1 regulates host cell apoptosis through the mitochondrial pathway and the death receptor pathway [ Microbiol Spectr, 2025, e0041625.] PubMed: 40853121
DBeQ derivative targets vacuolar protein sorting 4 functions in cancer cells and suppresses tumor growth in mice [ J Pharmacol Exp Ther, 2025, 392(4):103524] PubMed: 40147096
Sodium silicate complex reduces subdermal hemorrhage and prolongs survival after envenomation by Trimeresurus stejnegeri stejnegeri [ Toxicon, 2025, 265:108495] PubMed: 40669755
EFHD2 suppresses intestinal inflammation by blocking intestinal epithelial cell TNFR1 internalization and cell death [ Nat Commun, 2024, 15(1):1282] PubMed: 38346956
PARP inhibitors enhance antitumor immune responses by triggering pyroptosis via TNF-caspase 8-GSDMD/E axis in ovarian cancer [ J Immunother Cancer, 2024, 12(10)e009032] PubMed: 39366751
RIPK1 is dispensable for cell death regulation in β-cells during hyperglycemia [ Mol Metab, 2024, 87:101988] PubMed: 39004142

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。