CAS NO: | 210345-04-3 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
Molecular Weight (MW) | 690.72 |
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Formula | C32H43FN6O10 |
CAS No. | 210345-04-3 (free base); |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: ≥ 10mg/mL |
Water: N/A | |
Ethanol: N/A | |
Chemical Name | methyl (4S)-5-[[(2S)-1-[[(3S)-5-fluoro-1-methoxy-1,4-dioxopentan-3-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-[[(2S)-4-methyl-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-5-oxopentanoate |
Synonyms | Z-LEHD-FMK; Z-LEHD-FMK; Z LEHD-FMK; Z LEHD FMK; Z-LEHD FMK |
SMILES Code | CC(C)CC(C(=O)NC(CCC(=O)OC)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)OCC2=CC=CC=C2 |
Target | Caspase-9 |
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In Vitro | Z-LEHD-FMK (20 μM; pretreated for 30 min) completely protects HCT116 and 293 cells from TRAIL-induced toxicity[1]. Z-LEHD-FMK (20 μM ; 6 h) protects normal human hepatocytes from TRAIL-induced apoptosis[1]. Apoptosis Analysis[1] Cell Line: SW480, H460, HCT116 and 293 cells Concentration: 20 μM Incubation Time: Pretreated for 30 min Result: Protected HCT116 and 293 cells from TRAIL-induced apoptosis. Western Blot Analysis[1] Cell Line: HCT116, SW480 cells Concentration: 20 μM Incubation Time: 2 h Result: Protected procaspase 3 from cleavage in HCT116 cells but not in SW480 cells, especially at the 16-h time point. |
In Vivo | Z-LEHD-FMK (0.8 μmol/kg; i.v. for 7 d) protects neurons, glia, myelin, axons, and intracellular organelles in spinal cord injury (SCI) rats[2]. Animal Model: Male Wistar albino rats (250-350 g) with SCI[2] Dosage: 0.8 μmol/kg Administration: I.v. for 1 or 7 days Result: Decreased the mean apoptotic cell count at 24 hours and 7 days postinjury. |
References | [1]. 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]. 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]. Caspase inhibition and limitation of myocardial infarct size: protection against lethal reperfusion injury. Br J Pharmacol. 2000 May; 130(2): 197-200. |