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Synonyms | Caspase-3 Inhibitor | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C30H41FN4O12 |
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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) |
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* <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. |
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. |
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in vitro | Z-DEVD-FMK (1–200 μM) inhibits D4-GDI cleavage and apoptosis in a concentration-dependent manner. [1] Z-DEVD-FMK reduces ceramide-induced cardiomyocyte death and significantly inhibits the activation of caspase 3. [3] Z-DEVD-FMK (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] Z-DEVD-FMK (100 μM) blocks MPP+-induced increases in caspase-3 enzyme activity. Z-DEVD-FMK 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] |
キナーゼアッセイ | Caspase activity assay | |
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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 |
, , 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.]
Pyroptotic T cell-derived active IL-16 has a driving function in ovarian endometriosis development [ Cell Rep Med, 2024, 5(3):101476] | PubMed: 38508138 |
Induction of IFIT1/IFIT3 and inhibition of Bcl-2 orchestrate the treatment of myeloma and leukemia via pyroptosis [ Cancer Lett, 2024, 588:216797] | PubMed: 38462032 |
Chemical Hypoxia Induces Pyroptosis in Neuronal Cells by Caspase-Dependent Gasdermin Activation [ Int J Mol Sci, 2024, 25(4)2185] | PubMed: 38396860 |
Carboxypeptidase A4 negatively regulates HGS-ETR1/2-induced pyroptosis by forming a positive feedback loop with the AKT signalling pathway [ Cell Death Dis, 2023, 14(12):793] | PubMed: 38049405 |
Antileukemic effect of venetoclax and hypomethylating agents via caspase-3/GSDME-mediated pyroptosis [ J Transl Med, 2023, 21(1):606] | PubMed: 37679782 |
Antileukemic effect of venetoclax and hypomethylating agents via caspase-3/GSDME-mediated pyroptosis [ J Transl Med, 2023, 21(1):606] | PubMed: 37679782 |
FAP is critical for ovarian cancer cell survival by sustaining NF-κB activation through recruitment of PRKDC in lipid rafts [ Cancer Gene Ther, 2023, 30(4):608-621] | PubMed: 36494579 |
Immunostimulatory oncolytic activity of coxsackievirus A11 in human malignant pleural mesothelioma [ Cancer Sci, 2023, 114(3):1095-1107] | PubMed: 36369966 |
Pharmacological Targeting of Bcl-2 Induces Caspase 3-Mediated Cleavage of HDAC6 and Regulates the Autophagy Process in Colorectal Cancer [ Int J Mol Sci, 2023, 24(7)6662] | PubMed: 37047634 |
Protein engineering reveals that gasdermin A preferentially targets mitochondrial membranes over the plasma membrane during pyroptosis [ J Biol Chem, 2023, 299(2):102908] | PubMed: 36642180 |
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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