210344-98-2
210344-98-2 structure
- Name: Z-IETD-FMK
- Chemical Name: Methyl (5S,8S,11S,14S)-5-[(2S)-2-butanyl]-14-(fluoroacetyl)-11-[(1R)-1-hydroxyethyl]-8-(3-methoxy-3-oxopropyl)-3,6,9,12-tetraoxo-1-phenyl-2-oxa-4,7,10,13-tetraazahexadecan-16-oate
- CAS Number: 210344-98-2
- Molecular Formula: C30H43FN4O11
- Molecular Weight: 654.681
- Catalog: Peptides
- Create Date: 2018-06-11 19:35:32
- Modify Date: 2024-01-01 22:53:43
-
Z-IETD-FMK is a selective and cell permeable caspase 8 inhibitor.
| Name | Methyl (5S,8S,11S,14S)-5-[(2S)-2-butanyl]-14-(fluoroacetyl)-11-[(1R)-1-hydroxyethyl]-8-(3-methoxy-3-oxopropyl)-3,6,9,12-tetraoxo-1-phenyl-2-oxa-4,7,10,13-tetraazahexadecan-16-oate |
|---|---|
| Synonyms |
Methyl (5S,8S,11S,14S)-5-[(2S)-butan-2-yl]-14-(fluoroacetyl)-11-[(1R)-1-hydroxyethyl]-8-(3-methoxy-3-oxopropyl)-3,6,9,12-tetraoxo-1-phenyl-2-oxa-4,7,10,13-tetraazahexadecan-16-oate (non-preferred name)
Methyl (5S,8S,11S,14S)-5-[(2S)-2-butanyl]-14-(fluoroacetyl)-11-[(1R)-1-hydroxyethyl]-8-(3-methoxy-3-oxopropyl)-3,6,9,12-tetraoxo-1-phenyl-2-oxa-4,7,10,13-tetraazahexadecan-16-oate Z-IETD-FMK |
| Description | Z-IETD-FMK is a selective and cell permeable caspase 8 inhibitor. |
|---|---|
| Related Catalog | |
| Target |
Caspase-8 |
| In Vitro | Z-IETD-FMK causes full inhibition only of the proapoptotic effect of TNFα with an IC50 of 0.46 μM[1]. Z-IETD-FMK and Z-VAD-FMK at non-toxic doses are found to be immunosuppressive and inhibit human T cell proliferation induced by mitogens and IL-2. They are shown to block NF-κB in activated primary T cells, but have little inhibitory effect on the secretion of IL-2 and IFN-γ during T cell activation[2]. Z-IETD-FMK inhibits the cleavage of caspase-8 and only partially inhibits the cleavage of caspase-3 and PARP. Z-IETD-FMK can prevent the execution of apoptosis in retinal cells exposed to different apoptotic stimuli[3]. |
| In Vivo | Pharmacological inhibition of caspase-8 by z-IETD-FMK robustly reduces tumour outgrowth and this is closely associated with a reduction in the release of pro-inflammatory cytokines, IL-6, TNF-α, IL-18, IL-1α, IL-33, but not IL-1β. Furthermore, inhibition of caspase-8 reduces the recruitment of innate suppressive cells, such as myeloid-derived suppressor cells, but not of regulatory T cells to lungs of tumour-bearing mice[4]. |
| Cell Assay | T cell proliferation following mitogen stimulation is determined using [3H]-thymidine incorporation. In brief, PBMCs or purified T cells are seeded at 1×106 cells/mL in 96 well plates and stimulated with either PHA (5 μg/mL or co-stimulated with anti-CD3 mAb (5 μg/mL) and anti-CD28 mAb (2.5 μg/mL) in the presence or absence of caspase inhibitor Z-IETD-FMK. The cells are cultured for 72 h with the last 16 h pulsed with [[3H]-labelled methyl-thymidine (0.037 MBq) prior to harvest onto glass fibre filter mats using a Tomtec automated multi-well harvester[2]. |
| Animal Admin | Mice: Mice are divided into three groups: (1) naive, non-treated, mice; (2) CTR (control), i.t. instilled with NMU; and (3) lung cancer-bearing mice treated with Z-IETD-FMK (0.5 μg per mouse). The involvement of caspase-8 in lung cancer development is the determined at different time points (3, 7 and 28 days)[4]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 925.7±65.0 °C at 760 mmHg |
| Molecular Formula | C30H43FN4O11 |
| Molecular Weight | 654.681 |
| Flash Point | 513.6±34.3 °C |
| Exact Mass | 654.291260 |
| LogP | 3.92 |
| Vapour Pressure | 0.0±0.3 mmHg at 25°C |
| Index of Refraction | 1.518 |
| Storage condition | -20°C |