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Z-DEVD-FMK
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Screening Libraries
Cat. No.: HY-12466
CAS No.: 210344-95-9
Molecular Formula: C₃₀H₄₁FN₄O₁₂
Molecular Weight: 668.66
Target: Caspase
Pathway: Apoptosis
•
Proteins
Storage: Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Mass
Solvent 1 mg 5 mg 10 mg
Concentration
Preparing
1 mM 1.4955 mL 7.4776 mL 14.9553 mL
Stock Solutions
5 mM 0.2991 mL 1.4955 mL 2.9911 mL
In Vivo 1. Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline
Solubility: ≥ 1 mg/mL (1.50 mM); Clear solution
2. Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1 mg/mL (1.50 mM); Clear solution
BIOLOGICAL ACTIVITY
Description Z-DEVD-FMK is a specific and irreversible caspase-3 inhibitor with an IC50 of 18 μM[1].
In Vitro N27 cells are exposed to MPP+ in the absence or presence of 50 μM Z-DIPD-FMK or 100 μM Z-DEVD-FMK or 50 μM Z-LEHD-FMK
and then caspase-9 and caspase-3 enzymatic activities are determined by enzymatic assay at 12 and 24 h following
exposure, respectively. Exposure to 300 μM MPP+ for 24 h in N27 cells results in an approximately 2.5-fold increase in
caspase-3 enzyme activity. MPP+-induced increases in caspase-3 enzyme activity are significantly blocked by 50 μM Z-DIPD-
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FMK, 100 μM Z-DEVD-FMK, and 50 μM Z-LEHD-FMK[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo Early Z-DEVD-FMK (160 ng) treatment improves motor and cognitive function after traumatic CNS injury induced by severe
controlled cortical impact (CCI) in the mouse[2]. Treatment with Z-DEVD-FMK (160 ng) significantly improves neurological
outcome when compared with traumatized animals treated with DMSO vehicle (p<0.01)[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
PROTOCOL
Cell Assay [1] N27 cells and primary mesencephalic neurons are exposed to either 10-100 μM 6-OHDA or 10-300 μM MPP+ in the presence
or absence of 0.1-50 μM Z-DIPD-FMK or 0.1-100 μM Z-DEVD-FMK or 50 μM Z-IETD-FMK or Z-LEHD-FMK for the duration of the
experiment. 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 μ
M Z-DEVD-FMK and cell death is determined by MTT 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[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Mice[2]
Administration [2][3] Male C57Bl/6 mice (20-25 g) are used. For treatment with Z-DEVD-fmk or vehicle after CCI, mice are placed in a stereotaxic
apparatus, and the CCI wound is reopened for intracerebroventricular injection. Either Z-DEVD-FMK (160 ng in 2 μL DMSO),
or DMSO vehicle is injected over a 5-minute period.
Rats[3]
Male Sprague Dawley rats (425±25 g) are used. DMSO (5 μL) vehicle or Z-DEVD-FMK (160 ng in 5 μL of DMSO) is administered
at a controlled rate of 0.5 μL/min via an infusion pump at 30 min before and at 6 and 24 hr after TBI. At the designated time
periods after injury, animals are decapitated under NSC 10816 anesthesia (100 mg/kg, i.p.), and the brains are removed
rapidly and dissected. Sham-operated (control) animals received anesthesia and surgery but are not subjected to trauma.
Tissue samples are collected 1, 4, 12, 24, and 72 hr after TBI. Samples are frozen on dry ice and kept at −85°C.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
CUSTOMER VALIDATION
REFERENCES
[1]. Kanthasamy AG, et al. A novel peptide inhibitor targeted to caspase-3 cleavage site of a proapoptotic kinase protein kinase C delta (PKCdelta) protects against
dopaminergic neuronal degeneration in Parkinson's disease models. Free Radic Biol Med. 2006 Nov
[2]. Knoblach SM, et al. Caspase inhibitor z-DEVD-fmk attenuates calpain and necrotic cell death in vitro and after traumatic brain injury. J Cereb Blood Flow Metab. 2004
Oct;24(10):1119-32.
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[3]. Yakovlev AG, et al. Activation of CPP32-like caspases contributes to neuronal apoptosis and neurological dysfunction after traumatic brain injury. J Neurosci. 1997,
17(19), 7415-7424.
[4]. Huang MY, et al. Chemotherapeutic agent CPT-11 eliminates peritoneal resident macrophages by inducing apoptosis. Apoptosis. 2016 Feb;21(2):130-42.
McePdfHeight
Caution: Product has not been fully validated for medical applications. For research use only.
Page 3 of 3 www.MedChemExpress.com
Inhibitors
Certificate of Analysis
Z-DEVD-FMK
•
Screening Libraries
Cat. No.: HY-12466
CAS No.: 210344-95-9
Batch No.: 264908
Chemical Name: L-Valinamide, N-[(phenylmethoxy)carbonyl]-L-α-aspartyl-L-α-glutamyl-N-[(1S)-3-fluoro-1-(2-me
thoxy-2-oxoethyl)-2-oxopropyl]-, 1,2-dimethyl ester
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PHYSICAL AND CHEMICAL PROPERTIES
Proteins
Molecular Formula: C30H41FN4O12
Molecular Weight: 668.66
Storage: Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Chemical Structure:
ANALYTICAL DATA
Appearance: White to off-white (Solid)
1H NMR Spectrum: Consistent with structure
Conclusion: The product has been tested and complies with the given specifications.
Caution: Product has not been fully validated for medical applications. For research use only.
Page 1 of 1 www.MedChemExpress.com
Safety Data Sheet
Inhibitors
Revision Date: Mar.-30-2021
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Print Date: Feb.-25-2023
Screening Libraries
1. PRODUCT AND COMPANY IDENTIFICATION
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CAS No. : 210344-95-9
Proteins
1.2 Relevant identified uses of the substance or mixture and uses advised against
Identified uses : Laboratory chemicals, manufacture of substances.
1.3 Details of the supplier of the safety data sheet
Company: MedChemExpress USA
Tel: 609-228-6898
Fax: 609-228-5909
E-mail: sales@medchemexpress.com
1.4 Emergency telephone number
Emergency Phone #: 609-228-6898
2. HAZARDS IDENTIFICATION
Pictogram
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Continue rinsing.
2.3 Other hazards
None.
3. COMPOSITION/INFORMATION ON INGREDIENTS
3.1 Substances
Formula: C30H41FN4O12
Molecular Weight: 668.66
CAS No. : 210344-95-9
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6.2 Environmental precautions
Try to prevent further leakage or spillage. Keep the product away from drains or water courses.
6.3 Methods and materials for containment and cleaning up
Absorb solutions with finely-powdered liquid-binding material (diatomite, universal binders); Decontaminate surfaces and
equipment by scrubbing with alcohol; Dispose of contaminated material according to Section 13.
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Melting/freezing point No data available
Boiling point/range No data available
Flash point No data available
Evaporation rate No data available
Flammability (solid, gas) No data available
Upper/lower flammability or explosive limits No data available
Vapor pressure No data available
Vapor density No data available
Relative density No data available
Water Solubility No data available
Partition coefficient No data available
Auto-ignition temperature No data available
Decomposition temperature No data available
Viscosity No data available
Explosive properties No data available
Oxidizing properties No data available
9.2 Other safety information
No data available.
11.TOXICOLOGICAL INFORMATION
11.1 Information on toxicological effects
Acute toxicity
Classified based on available data. For more details, see section 2
Skin corrosion/irritation
Classified based on available data. For more details, see section 2
Serious eye damage/irritation
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Classified based on available data. For more details, see section 2
Respiratory or skin sensitization
Classified based on available data. For more details, see section 2
Germ cell mutagenicity
Classified based on available data. For more details, see section 2
Carcinogenicity
IARC: No component of this product present at a level equal to or greater than 0.1% is identified as probable, possible or
confirmed human carcinogen by IARC.
ACGIH: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed
carcinogen by ACGIH.
NTP: No component of this product present at a level equal to or greater than 0.1% is identified as a anticipated or confirmed
carcinogen by NTP.
OSHA: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed
carcinogen by OSHA.
Reproductive toxicity
Classified based on available data. For more details, see section 2
Specific target organ toxicity - single exposure
Classified based on available data. For more details, see section 2
Specific target organ toxicity - repeated exposure
Classified based on available data. For more details, see section 2
Aspiration hazard
Classified based on available data. For more details, see section 2
Additional information
This information is based on our current knowledge. However the chemical, physical, and toxicological properties have not been
completely investigated.
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13.1 Waste treatment methods
Product
Dispose substance in accordance with prevailing country, federal, state and local regulations.
Contaminated packaging
Conduct recycling or disposal in accordance with prevailing country, federal, state and local regulations.
IMDG
Proper shipping name: Not dangerous goods
UN number: -
Class: -
Packing group: -
IATA
Proper shipping name: Not dangerous goods
UN number: -
Class: -
Packing group: -
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harm.
Caution: Product has not been fully validated for medical applications. For research use only.
Page 7 of 7 www.MedChemExpress.com
CAS NO.: 210344-95-9 , CD3OD
Parameter Value
7.372
7.356
7.339
7.319
7.310
7.304
7.297
7.288
5.208
5.171
5.130
5.107
5.091
5.054
4.834
4.744
4.525
4.508
4.492
4.418
4.378
4.300
4.128
4.114
4.096
3.669
3.663
3.646
3.614
3.314
3.310
3.306
3.302
3.298
2.939
2.924
2.792
2.768
2.750
2.427
0.967
0.955
0.950
0.938
1 Title
2 Comment
3 Origin Bruker BioSpin
GmbH
4 Owner nmrsu
5 Site
6 Spectrometer Avance
7 Author
8 Solvent MeOD
9 Temperature 300.0
10 Pulse Sequence zg30
11 Experiment 1D
12 Number of 8
Scans
13 Receiver Gain 101
14 Relaxation 1.0000
Delay
15 Pulse Width 8.0000
16 Acquisition 3.9977
Time
17 Acquisition 2023-05-05T15:
Date 04:28
18 Modification 2023-05-05T15:
Date 10:57
19 Spectrometer 400.13
Frequency
20 Spectral Width 8196.7
21 Lowest -1636.9
Frequency
22 Nucleus 1H
23 Acquired Size 32768
24 Spectral Size 65536
4.85
3.07
1.00
3.00
1.07
9.02
6.02
2.05
1.00
6.05
11 10 9 8 7 6 5 4 3 2 1 0 -1
f1 (ppm)