Catalog No. B3233

Z-LEHD-FMK

不可逆的Caspase-9抑制剂

规格	价格	货期	数量
1mg	￥2375.00	现货
5mg	￥6569.00	现货

CAS号：210345-04-3纯度：98.00%

仅用于科研，不用于诊疗。未经明确授权不得转售。

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特色产品

Annexin V-FITC/PI Apoptosis Kit

用于双染检测细胞凋亡和坏死

- 在10-20分钟内完成染色
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞

Phos binding reagent (Phosbind) acrylamide

分离和检测磷酸化/非磷酸化蛋白

- 新型的磷酸盐结合标签和功能分子
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白

Cell Counting Kit-8 (CCK-8)

用于细胞增殖和细胞毒性试验

- 比MTT，MTS或WST-1更敏感
- 对细胞无毒性
- 步骤更简单，无需有机溶剂

Cy5 TSA Fluorescence System Kit

Cy5荧光标记的酪胺信号放大系统

- 检测ICC/IHC/ISH中的低丰度靶点
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率

EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)

用于观察mRNA运送，定位，翻译

- 具有Cap1结构的荧光素酶mRNA
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰

HotStart™ 2X Green qPCR Master Mix

用于荧光定量目标DNA或cDNA

- 通过热启动机制优化扩增特异性
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单

HyperScribe™ T7 High Yield Cy5 RNA Labeling Kit Plus

高效的Cy5修饰RNA转录试剂盒

- 适合原位/Northernblot杂交实验
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量

产品描述产品性质产品应用生物相关数据质量控制操作说明产品引用文献摩尔浓度计算器

产品描述

Z-LEHD-FMK (CAS号210345-04-3) 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.

产品性质

物理外观	Solid
CAS号	210345-04-3
分子式	C₃₂H₄₃FN₆O₁₀
分子量	690.72
化学名称	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
溶解度	insoluble in H2O; ≥107.4 mg/mL in DMSO; ≥98.2 mg/mL in EtOH
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
存储条件	-20°C
运输条件	蓝冰

产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)

IC50和靶点

生物活性描述

Z-LEHD-FMK是一种选择性的强效caspase-9抑制剂，可防止再灌注损伤并延缓细胞凋亡。Z-LEHD-FMK具有抗肿瘤和神经保护活性，能提高体外培育的小黄牛胚胎植入前的产量，并能改变细胞的应激反应。

生物相关数据

质量控制

请选择批次查看:

纯度 = 98.00%

COA (Certificate Of Analysis)MS (Mass Spectrometry)MSDS (Material Safety Data Sheet)

操作说明

小分子化合物通用使用指南 Datasheet

APExBIO 顾客使用本产品发表的 21 篇科研文献

1. Maria Landherr, Iuliia Polina, et al. "SARS-CoV-2-ORF3a variant Q57H reduces its pro-apoptotic activity in host cells." F1000Res. 2025 Nov 22;13:331. PMID: 41480481

2. Ravi Padia, Lei Sun, et al. "HOXC8 impacts lung tumorigenesis by preventing pyroptotic cell death through the suppression of caspase-1 expression." Cell Death Dis. 2025 Jul 23;16(1):552. PMID: 40701951

3. Wumei Zhao, Ziwen Chen, et al. "Induction of apoptosis and hypoxic stress in malignant melanoma cells via graphene-mediated far-infrared radiation." BMC Cancer 25, 620 (2025) PMID: 40197161

4. Maria Landherr, Iuliia Polina, et al. "SARS-CoV-2-ORF3a variant Q57H reduces its pro-apoptotic activity in host cells." F1000Research 2024

5. Zhi Chen, He Chang, et al. "Chicken GSDME, a major pore-forming molecule responsible for RNA virus-induced pyroptosis in chicken." Veterinary Microbiology Research Article 22 November 2024

6. Yuhang Miao, Tao Ding, et al. "The Yeast and Hypha Phases ofCandida kruseiInduce the Apoptosis of Bovine Mammary Epithelial Cells via Distinct Signaling Pathways." Animals (Basel). 2023 Oct 15;13(20):3222. PMID: 37893947

7. Wumei Zhao, Chengyun Zhang, et al. "Graphene as a nanomaterial induces apoptosis and hypoxic stress in melanoma cells." Research Square. 12 Oct, 2023

8. Claire Reynolds-Peterson, Dylan J Ehrbar, et al. "Sensitization of Airway Epithelial Cells to Toxin-Induced Death by TNF Superfamily Cytokines." Methods Mol Biol. 2021;2248:19-42. PMID: 33185865

9. Yaling Zhai, Youxia Liu, et al. "The soluble VEGF receptor sFlt-1 contributes to endothelial dysfunction in IgA nephropathy." PLoS One. 2020 Aug 13;15(8):e0234492. PMID: 32790760

10. Zhao M, Duan X, et al. "A Novel Role for PX, a Structural Protein of Fowl Adenovirus Serotype 4 (FAdV4), as an Apoptosis-Inducer in Leghorn Male Hepatocellular Cell." Cell. Viruses. 2020;12(2):E228. Published 2020 Feb 18. PMID: 32085479

11. Zhou J, Huang Z, et al. "Piperlongumine induces apoptosis and G2/M phase arrest in human osteosarcoma cells by regulating ROS/PI3K/Akt pathway." Toxicol In Vitro. 2020;65:104775. PMID: 31987842

12. Jiao C, Chen W, et al. "Ganoderma lucidum spore oil induces apoptosis of breast cancer cells in vitro and in vivo by activating caspase-3 and caspase-9." J Ethnopharmacol. 2019 Oct 3:112256. PMID: 31586690

13. Hodges AL, Kempen CG, et al. "TNF Family Cytokines Induce Distinct Cell Death Modalities in the A549 Human Lung Epithelial Cell Line when Administered in Combination with Ricin Toxin." Toxins (Basel). 2019 Aug 1;11(8). pii: E450. PMID: 31374990

14. Gan I, Jiang J, et al. "Mitochondrial permeability regulates cardiac endothelial cell necroptosis and cardiac allograft rejection." Am J Transplant. 2018 Sep 11. PMID: 30203531

15. Song F, Yu X, et al. "Caspase-3 Inhibition Attenuates the Cytopathic Effects of EV71 Infection. Front Microbiol." 2018 Apr 26;9:817. PMID: 29755438

16. Wang JN, Zhang ZR, et al. "Acetyl-macrocalin B, an ent-kaurane diterpenoid, initiates apoptosis through the ROS-p38-caspase 9-dependent pathway and induces G2/M phase arrest via the Chk1/2-Cdc25C-Cdc2/cyclin B axis in non-small cell lung cancer." Cancer Biol Ther. 2018 Jul 3;19(7):609-621. PMID: 29565730

17. Wang J, Zhang Z, et al. "Rabdocoestin B exhibits antitumor activity by inducing G2/M phase arrest and apoptosis in esophageal squamous cell carcinoma." Cancer Chemother Pharmacol. 2018 Mar;81(3):469-481. PMID: 29308536

18. Yazhong Ge, Qing Gao, et al. "Su Yang Decoction induces human colon carcinoma cell apoptosis by activating caspases." Oncology letters.October 26, 2018

19. Wang F, Wei ZL, et al. "Apoptosis Inducing Factor Is Involved in Stretch-Induced Apoptosis of Myoblast via a Caspase-9 Independent Pathway." J Cell Biochem. 2016 Oct 13. PMID: 27735993

20. Chen Y, Sun M, et al. "SM-1, a novel PAC-1 derivative, activates procaspase-3 and causes cancer cell apoptosis." Cancer Chemother Pharmacol. 2016 Aug 3. PMID: 27488460

21. Tian, Chongchong, et al. "A novel dual EGFR/HER2 inhibitor KU004 induces cell cycle arrest and apoptosis in HER2-overexpressing cancer cells." Apoptosis 20.12 (2015): 1599-1612. PMID: 26437915

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