Z-DEVD-FMK

製品コードS7312 バッチS731204

印刷

化学情報

Chemical Structure Synonyms Caspase-3 Inhibitor Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C30H41FN4O12
分子量 668.66 CAS No. 210344-95-9
Solubility (25°C)* 体外 DMSO 100 mg/mL (149.55 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
2%DMSO 30%PEG400 5%Tween80 63%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。

 1.000mg/ml (1.50mM) Taking the 1 mL working solution as an example, add 20 μL of 50 mg/ml clarified DMSO stock solution to 300 μL of PEG 400, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 630 μL 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-DEVD-FMK (Caspase-3 Inhibitor) is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.
in vitro Z-DEVD-FMK (1–200 μM) inhibits D4-GDI cleavage and apoptosis in a concentration-dependent manner. [1] This compound reduces ceramide-induced cardiomyocyte death and significantly inhibits the activation of caspase 3. [3] It (100μM) attenuates OxyHb-induced cell detachment, reduced caspase-2 and -3 activities, abolishes OxyHb-induced DNA ladders, and prevents OxyHb-induced cleavage of PARP in cultured brain microvessel endothelial cells. [4] This chemical (100 μM) blocks MPP+-induced increases in caspase-3 enzyme activity. It dose dependently blocks 6-OHDA-induced apoptotic cell death with IC50 of 18 μM. [5]
in vivo Z-DEVD-FMK, before and after injury, markedly reduces post-traumatic apoptosis, and significantly improved neurological recovery. [2]

プロトコル(参考用のみ)

キナーゼアッセイ Caspase activity assay
Caspase-3 and caspase-9 activities are measured using fluorescent-based substrate. After treatment, the cells are resuspended in lysis buffer (50 mM Tris HCl, 1 mM EDTA, and 10 mM EGTA) containing 10 mM digitonin for 20 min at 37°C. Supernatants are treated with either of the fluorogenic substrates Ac-DEVD-AFC for caspase-3 or Ac-LEHD-AFC for caspase-9 for 1 h at 37°C and fluorescence is measured at excitation at 400 nm and emission at 505 nm using a Gemini XS fluorescence plate reade
細胞アッセイ 細胞株 N27 cells
濃度 ~50 μM
反応時間 24 hours
実験の流れ N27 cells are incubated with 100 μM 6-OHDA for 24 h or 300 μM MPP+ for 36 h in the presence or absence of 50 μM Z-DEVD-FMK and cell death is determined by MTT (3-(4,5-dimethylthiazol-3-yl)-2,5-diphenyl tetrazolium bromide) assay, which is widely used to assess cell viability. After treatment, the cells are incubated in serum-free medium containing 0.25 mg/ml MTT for 3 h at 37°C. Formation of formazan from tetrazolium is measured at 570 nm with a reference wavelength at 630 nm using a SpectraMax microplate reader.
動物実験 動物モデル Male Sprague Dawley rats with Brain trauma.
投薬量 160 ng
投与方法 Intracerebroventricular administration

参考

  • https://pubmed.ncbi.nlm.nih.gov/9485209/
  • https://pubmed.ncbi.nlm.nih.gov/9295387/
  • https://pubmed.ncbi.nlm.nih.gov/10997751/
  • https://pubmed.ncbi.nlm.nih.gov/11157197/
  • https://pubmed.ncbi.nlm.nih.gov/17045926/

カスタマーフィードバック

, , Mol Carcinog, 2016, 56(1):218-231

Data from [Data independently produced by , , Oncotarget, 2017, 8(2):3396-3411]

Data from [Data independently produced by , , INTERNATIONAL JOURNAL OF ONCOLOGY, 2016, 48:1710-1720.]

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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。

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