Z-DEVD-FMK

For research use only.

Catalog No.S7312 Synonyms: Caspase-3 Inhibitor

36 publications

Z-DEVD-FMK Chemical Structure

Molecular Weight(MW): 668.66

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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Selleck's Z-DEVD-FMK has been cited by 36 publications

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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
Caspase-3 [1]
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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
duck embryo fibroblasts (DEFs) MonUSpVv[3Srb36gZZN{[Xl? NX[zeFVNOiCqwrC= NYDrdmU3\W[oZXP0bZZmdHlicILvcY91\WRidnnyZYwhemWybHnjZZRqd25? MXmzNFgyOzVyMB?=
OSCC cell NGD1OplCeG:ydH;zbZMh[XO|YYm= NFfpXlQzOCEEtV2= MlOzOFghcA>? M4TJNJJm\HWlZTD0bIUh[WO2aY\peJkhd2ZiY3HzdIF{\SB|IHHu[EBk[XOyYYPlJFk> MoLUN|A2PzN7N{i=
A549 M3:0NGZ2dmO2aX;uJIF{e2G7 NVmyPXRQOjVizszN NEDWVZYzPCCq NV\mc29be2mpbnnmbYNidnSueTDpcohq[mm2IGLPV{Bo\W6ncnH0bY9vKGmwIFG1OFkh[2WubIO= M2PGXVMxOjRyN{C5
HCT116 cells NIT1eGdHfW6ldHnvckBie3OjeR?= NIWxWGw2OOLCid88US=> MWKyJIg> MUPjc5Rz\WG2bXXueEB4cXSqIGj5cI9xcW6nIITvJJBz\X[nboTlJJRp\SC6eXzvdIlv\S2rbnT1Z4VlKGmwY4LlZZNqdmdiYYDvdJRwe2m| MWiyPVM3OjZ4Nx?=
K562 cells M{faR2Z2dmO2aX;uJIF{e2G7 NXz6NlNjOiCq NGfxWIxqdmO{ZXHz[YQhWi5idnXycolkcW[udXGg[Zh1emGldD3pcoR2[2WmIHPlcIwheHKxbHnm[ZJifGmxbh?= NUe0XIZ{Ojl|MkizPFc>
THP-1 cells MX;GeY5kfGmxbjDhd5NigQ>? M3vKXVUxKM7:TR?= NXj0OodXOiCq M3zIUpN2[i2JMTDw[YFsKEmwaHnibZRqd25iaX6gSG1SSSCrbnT1Z4VlKGOnbHyg[IVifGh? M{jZd|I6OjJ3MUO2

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
HAUSP / Kinesin 5B / GEP100 / SDCCAG3 / PARD3 / Lamin A/C / PARP ; 

PubMed: 24195789     


HeLa cells were treated with 1 μM STS for 24 hr in the presence or absence of the 100 μM caspase inhibitors (Z-VEID-FMK; caspase-6 inhibitor, Z-DEVD-FMK; caspase-3/-7 inhibitor, Z-VAD-FMK; pan-caspase inhibitor) pretreated to cells for 3 hr. After 24 hr, 䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뾠Ղ䐺痖暼瘿뾠Ղᾰƌ 뾠Ղà㺣痖뾠Ղ€𢡄뾤Ղ€䀷痗뾤Ղ౴뾤Ղ㵶痗뾤Ղ뺖᎒泌Itemｾ᎒

CLK3 / ADH4 / MDH1; 

PubMed: 24195789     


HeLa cells were treated with 1 μM STS for 24 hr in the presence or absence of the 100 μM caspase inhibitors (Z-VEID-FMK; caspase-6 inhibitor, Z-DEVD-FMK; caspase-3/-7 inhibitor, Z-VAD-FMK; pan-caspase inhibitor) pretreated to cells for 3 hr. After 24 hr, 䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ෆĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ⟸෕䐺痖暼

ORF57 / caspase 7 / caspase 3; 

PubMed: 20159985     


Inhibition of ORF57 cleavage by specific caspase inhibitors. BCBL-1 cells treated with VA in the presence of 50 μmpeptide-based caspase inhibitors, including pan-caspase inhibitor z-VAD-fmk, caspase-3/7 inhibitor z-DEVD-fmk , caspase-3/6 inhibitor z-VEID-䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ෆĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ

24195789 20159985
In vivo Z-DEVD-FMK, before and after injury, markedly reduces post-traumatic apoptosis, and significantly improved neurological recovery. [2]

Protocol

Kinase Assay:[5]
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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 Research:[5]
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  • 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.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Male Sprague Dawley rats with Brain trauma.
  • Dosages: 160 ng
  • Administration: Intracerebroventricular administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (149.55 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 400+5% Tween 80+ddH2O
For best results, use promptly after mixing. 		1mg/mL

* 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 Information

Molecular Weight 668.66
Formula

C30H41FN4O12
CAS No. 210344-95-9
Storage powder
in solvent
Synonyms Caspase-3 Inhibitor
Smiles COC(=O)CCC(CC(=O)C(CC(=O)OC)NC(=O)OCC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)NC(CC(=O)OC)C(=O)CF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID