Name: Z-LEHD-FMK
Price: 300.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    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].
    
    [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.
- Properties
  - Alternative 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
    
    CAS Number
    
    210345-04-3
    
    Molecular Formula
    
    C32H43FN6O10
    
    Molecular Weight
    
    690.72
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥107.4 mg/mL in DMSO; ≥98.2 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. 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
    2. 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. PMID:32085479
    3. 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
    4. 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
    5. 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
    6. Yazhong Ge, Qing Gao, et al . "Su Yang Decoction induces human colon carcinoma cell apoptosis by activating caspases." Oncology letters.October 26, 2018.
    7. 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
    8. 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
    9. 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
    10. 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
    11. 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
    12. 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 Sep;78(3):643-54. PMID:27488460
    13. 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

Z-LEHD-FMK

Z-LEHD-FMK

Background

We Also Recommend

Almorexant

Betrixaban

XCT790