Z-LEHD-FMK
目录号 : GC16990
Z-LEHD-FMK 是一种选择性且不可逆的 caspase-9 抑制剂，可防止致命的再灌注损伤并减轻细胞凋亡。
Cas No.:210345-04-3
Sample solution is provided at 25 µL, 10mM.
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Z-LEHD-FMK is a specific and irreversible inhibitor of caspase-9 [1].
Caspase-9 is an initiator caspase and plays an important role in the mitochondrial death pathway. Caspase-9 is activated during programmed cell death and cleaves procaspase-7 and procaspase-3.
Z-LEHD-FMK is a specific and irreversible caspase-9 inhibitor. In HCT116 human colon cancer cell line and 293 human embryonic kidney cell line, Z-LEHD-FMK inhibited apoptosis mediated by tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). These results suggested that TRAIL induced death through the mitochondrial pathway in some human cells. In a colony assay, Z-LEHD-FMK inhibited the reduction of colony growth of HCT116 induced by TRAIL. In normal human hepatocytes, Z-LEHD-FMK protected cells from TRAIL-induced apoptosis. These results suggested that a combination of Z-LEHD-FMK and TRAIL selectively killed cancer cells while protecting normal liver cells [1].
In rats with focal ischemia/reperfusion, Z-LEHD-FMK improved neurological outcome by 63% and reduced infarction volume by 49% [2]. In spinal cord trauma rat model, Z-LEHD-FMK reduced apoptotic cell count and protected neurons, myelin, axons, glia and intracellular organelles in the spinal cord [3].
References:
[1]. Ozoren N, Kim K, Burns TF, 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, 60(22): 6259-6265.
[2]. Mouw G, Zechel JL, Zhou Y, et al. Caspase-9 inhibition after focal cerebral ischemia improves outcome following reversible focal ischemia. Metab Brain Dis, 2002, 17(3): 143-151.
[3]. Colak A, Karaoğlan A, Barut S, 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, 2(3): 327-334.
| Cell experiment [1]: | |
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Cell lines |
Human colon cancer, HCT116, human embryonic fibroblastand 293 cell lines |
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Preparation method |
Soluble in DMSO > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
20 μM Z-LEHD-FMK for 30 mins followed by 20ng/ml TRAIL for 4 hours |
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Applications |
Z-LEHD-FMK completely protects HCT116 and 293 cells from TRAIL-induced toxicity. Z-LEHD-FMK also protected human hepatocytes from TRAIL-induced apoptosis. The colony growth of HCT116 is reduced in the presence of TRAIL, and there are significantly more colonies present when the HCT116 cells were incubated in the presence of TRAIL and Z-LEHD-FMK. |
| Animal experiment [2]: | |
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Animal models |
Adult male Wistar albino rats, 250 to 350 g, spinal cord injury model |
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Dosage form |
Intravenous 0.8-mM/kg injection of z-LEHD-fmk. |
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Preparation method |
Dry-form z-LEHD-fmk was dissolved in dimethylsulfoxide prepared with phosphatebuffered saline. |
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Applications |
At 24 hours post-injury, the mean apoptotic cell count in trauma-only controls was significantly higher than that in z-LEHD-fmk–treated group. Electron microscopy results also show Z-LEHD-FMK treatment protected neurons, glia, myelin, axons, and intracellular organelles. The specimens treated with z-LEHD-fmk displays significantly fewer apoptotic cells and diminished axonal demyelination. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Ozoren N, Kim K, Burns TF, 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, 60(22): 6259-6265. 2. Colak A, Karao lan A, Barut S, 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, 2(3): 327-334. | |
| Cas No. | 210345-04-3 | SDF | |
| 化学名 | 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 | ||
| Canonical SMILES | 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 | ||
| 分子式 | C32H43FN6O10 | 分子量 | 690.72 |
| 溶解度 | ≥ 107.4 mg/mL in DMSO, ≥ 98.2 mg/mL in EtOH | 储存条件 | Store at -20° C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.4478 mL | 7.2388 mL | 14.4776 mL |
| 5 mM | 0.2896 mL | 1.4478 mL | 2.8955 mL |
| 10 mM | 0.1448 mL | 0.7239 mL | 1.4478 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet