Z-DEVD-FMK

貨號 Cat. No.
S7312
規格 Size
5~200mg
品牌 Brand
Selleckchem

Description

 



Z-DEVD-FMK
Catalog No.S7312

Z-DEVD-FMK 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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Biological Activity







































Description Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.
Targets            
IC50            
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]
Features  

Protocol(Only for Reference)


Kinase Assay: [5]









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

Cell Assay: [5]





















Cell lines N27 cells
Concentrations ~50 μM
Incubation Time 24 hours
Method 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.

Animal Study: [2]

















Animal Models Male Sprague Dawley rats with Brain trauma.
Dosages 160 ng
Administration Intracerebroventricular administration

1


References


Chemical Information


Download Z-DEVD-FMK SDF


 

















Molecular Weight (MW) 668.66
Formula

C30H41FN4O12


CAS No. 210344-95-9















Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms Caspase-3 Inhibitor

 





















Solubility (25°C) * In vitro DMSO mg/mL (<1 mM)
Water mg/mL (<1 mM)
Ethanol mg/mL (<1 mM)
* <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.


 








Chemical Name L-​Valinamide, N-​[(phenylmethoxy)​carbonyl]​-​L-​α-​aspartyl-​L-​α-​glutamyl-​N-​[(1S)​-​3-​fluoro-​1-​(2-​methoxy-​2-​oxoethyl)​-​2-​oxopropyl]​-​, 1,​2-​dimethyl ester

 


 

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