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Z-DEVD-FMK Caspase-3 inhibitor

Cat.No.S7312

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.
Z-DEVD-FMK Caspase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 668.66

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
duck embryo fibroblasts (DEFs) Function assay 2 h  effectively promoted viral replication 30813500
OSCC cell Apoptosis assay 20 µM 48 h reduce the activity of caspase 3 and caspase 9 30573978
A549 Function assay 25 μM 24 h significantly inhibit ROS generation in A549 cells 30240709
HCT116 cells Function assay 50 μM 2 h cotreatment with Xylopine to prevente the xylopine-induced increasing apoptosis 29362667
K562 cells Function assay 2 h increased R. verniciflua extract-induced cell proliferation 29328387
THP-1 cells Function assay 50 μM 2 h sub-G1 peak Inhibition in DMQA induced cell death 29225136
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 668.66 Formula

C30H41FN4O12

Storage (From the date of receipt)
CAS No. 210344-95-9 Download SDF Storage of Stock Solutions

Synonyms Caspase-3 Inhibitor Smiles CC(C)C(C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)C(CCC(=O)OC)NC(=O)C(CC(=O)OC)NC(=O)OCC1=CC=CC=C1

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (149.55 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Caspase-3 [1]
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]
Kinase Assay
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
In vivo
Z-DEVD-FMK, before and after injury, markedly reduces post-traumatic apoptosis, and significantly improved neurological recovery. [2]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11157197/
  • [5] https://pubmed.ncbi.nlm.nih.gov/17045926/

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