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Z-LEHD-FMK TFA

Catalog No. T40602   CAS 524746-03-0

Z-LEHD-FMK TFA is a specific and irreversible inhibitor of caspase-9, offering protection against detrimental reperfusion injury and moderating apoptosis. Additionally, Z-LEHD-FMK TFA demonstrates its neuroprotective potential in a rat model of spinal cord trauma.

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Z-LEHD-FMK TFA Chemical Structure
Z-LEHD-FMK TFA, CAS 524746-03-0
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Z-LEHD-FMK TFA is a specific and irreversible inhibitor of caspase-9, offering protection against detrimental reperfusion injury and moderating apoptosis. Additionally, Z-LEHD-FMK TFA demonstrates its neuroprotective potential in a rat model of spinal cord trauma.
In vitro Z-LEHD-FMK at a concentration of 20 μM, when pretreated for 30 minutes, effectively shields HCT116 and 293 cells from TRAIL-induced toxicity and apoptosis [1]. Furthermore, this compound, when applied for 6 hours, safeguards normal human hepatocytes against TRAIL-induced apoptosis [1]. Apoptosis analysis indicates that a 20 μM concentration of Z-LEHD-FMK, following a 30-minute pretreatment, results in protection against TRAIL-induced apoptosis specifically in HCT116 and 293 cells [1]. Western blot analysis reveals that, at the same concentration and with a 2-hour incubation, Z-LEHD-FMK prevents the cleavage of procaspase 3 in HCT116 cells, showcasing its protective effect against apoptosis. However, this protective effect is not observed in SW480 cells, particularly notable at the 16-hour time point [1].
In vivo Z-LEHD-FMK (0.8 μmol/kg; i.v. for 7 d) exhibits neuroprotective properties in spinal cord injury (SCI) male Wistar albino rats (250-350 g), safeguarding neurons, glia, myelin, axons, and intracellular organelles[2]. Administered intravenously at a dosage of 0.8 μmol/kg for either 1 or 7 days, it significantly reduces the average apoptotic cell count at both 24 hours and 7 days following injury[2].
Molecular Weight 804.75
Formula C34H44F4N6O12
CAS No. 524746-03-0

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keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Ozoren N, et, al. The caspase 9 inhibitor Z-LEHD-FMK protects human liver cells while permitting death of cancer cells exposed to tumor necrosis factor-related apoptosis-inducing ligand. Cancer Res. 2000 Nov 15; 60(22): 6259-65. 2. Colak A, et, al. Neuroprotection and functional recovery after application of the caspase-9 inhibitor z-LEHD-fmk in a rat model of traumatic spinal cord injury. J Neurosurg Spine. 2005 Mar; 2(3): 327-34. 3. Mocanu MM, et, al. Caspase inhibition and limitation of myocardial infarct size: protection against lethal reperfusion injury. Br J Pharmacol. 2000 May; 130(2): 197-200.

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Keywords

Z-LEHD-FMK TFA 524746-03-0 ZLEHDFMK TFA Z LEHD FMK TFA inhibitor inhibit

 

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