Z-LEHD-FMK
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Z-LEHD-FMK是一种特异性的不可逆Caspase-9抑制剂[1]。
Caspase-9是一个起始caspase（initiator caspase），在线粒体介导的细胞死亡途径中起重要作用。在细胞凋亡过程中，Caspase-9被激活，并切割procaspase-7和procaspase-3。
Z-LEHD-FMK是一种特异性的不可逆Caspase-9抑制剂。在HCT116人结肠癌细胞系和293人胚肾细胞系中，Z-LEHD-FMK抑制TRAIL（tumor necrosis factor-related apoptosis-inducing ligand）介导的细胞凋亡，这些结果表明，TRAIL通过线粒体途径诱导细胞死亡。在集落形成实验中，Z-LEHD-FMK抑制TRAIL介导的HCT116集落生长的减少。在正常的人肝细胞中，Z-LEHD-FMK也可以抑制TRAIL诱导的细胞凋亡。这些结果表明，Z-LEHD-FMK和TRAIL共同作用可以选择性地杀死癌细胞，同时保护正常肝细胞[1]。
在局部缺血/再灌注的大鼠中，Z-LEHD-FMK可以改善63%的神经功能，并减少49%的梗死体积[2]。在脊髓创伤大鼠模型中，Z-LEHD-FMK减少脊髓中凋亡细胞的数量，保护神经元、髓鞘、轴突、神经胶质细胞和细胞内细胞器[3]。
参考文献：
[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, 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.
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| Storage | Store at -20°C |
| M.Wt | 690.72 |
| Cas No. | 210345-04-3 |
| Formula | C32H43FN6O10 |
| Solubility | insoluble in H2O; ≥107.4 mg/mL in DMSO; ≥98.2 mg/mL in EtOH |
| 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 |
| SDF | Download SDF |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验: [1] | |
|
细胞系 |
人结肠癌、HCT116、人胚胎成纤维细胞和293细胞系 |
|
制备方法 |
该化合物在DMSO中的溶解度大于10 mM，若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
|
反应条件 |
20 μM Z-LEHD-FMK 处理30 min后，使用20 ng/ml TRAIL处理4 hours |
|
实验结果 |
Z-LEHD-FMK完全保护HCT116和293细胞免受TRAIL诱导的毒性。Z-LEHD-FMK还保护人肝细胞免受TRAIL诱导的细胞凋亡。在TRAIL存在下，HCT116的集落生长减少，在TRAIL和Z-LEHD-FMK存在下孵育HCT116细胞产生更多的集落。 |
| 动物实验: [2] | |
|
动物模型 |
成年雄性Wistar白化大鼠，250?350 g，脊髓损伤模型 |
|
给药剂量 |
静脉内注射0.8 mM/kg z-LEHD-fmk |
|
制备方法 |
干的z-LEHD-fmk溶解在用磷酸盐缓冲盐水制备的二甲基亚砜中。 |
|
实验结果 |
在损伤后24小时，创伤组的平均凋亡细胞计数显著高于z-LEHD-fmk治疗组。电子显微镜结果表明，Z-LEHD-FMK保护神经元、神经胶质、髓磷脂、轴突和细胞内细胞器。用z-LEHD-fmk处理的标本具有显著更少的凋亡细胞，减少轴突脱髓鞘。 |
|
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
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. |
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质量控制和MSDS
- 批次:
化学结构
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