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Caspase-9 Inhibitor Z-LEHD-FMK
Novel and selective caspase-9 inhibitor

Catalog No.B4573
Size Price Stock Qty
100 µl (2 mM)
$125.00
In stock
20 µl (10 mM)
$125.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

      

Sample solution is provided at 25 µL, 10mM.

Product Citations

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

Quality Control

Quality Control & MSDS

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Chemical structure

Caspase-9 Inhibitor Z-LEHD-FMK

Protocol

Cell experiment [1]:

Cell lines

HCT116 cells, SW480 cells and human hepatocytes

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

20 μM

Applications

Pretreatment with Z-LEHD-FMK for 30 mins protected HCT116 cells but not SW480 cells from TRAIL-induced apoptosis. In human hepatocytes, the treatment with Z-LEHD-FMK and TRAIL for 6 hrs significantly reduced TRAIL-mediated toxicity. Thus, it was implied that Z-LEHD-FMK in combination with TRAIL selectively killed some cancer cells while protecting the liver.

Animal experiment [2]:

Animal models

A rat model of traumatic spinal cord injury

Dosage form

0.8 μM/kg; i.v.

Applications

In rat models of traumatic spinal cord injury, immediate treatment with Z-LEHD-FMK significantly inhibited post-spinal cord injury (SCI) apoptosis by blocking caspase-9 action in the apoptosis pathway. Moreover, electron microscopy findings confirmed that Z-LEHD-FMK protected neurons, glia, myelin, axons as well as intracellular organelles.

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.

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, Karaolan 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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Chemical Properties

Cas No. N/A SDF Download SDF
Chemical Name (Z)-2-((Z)-(2-((E)-((benzyloxy)(hydroxy)methylene)amino)-1-hydroxy-4-methylpentylidene)amino)-N-((Z)-1-((5-fluoro-1-methoxy-1,4-dioxopentan-3-yl)imino)-1-hydroxy-3-(1H-imidazol-5-yl)propan-2-yl)-5-methoxy-5-oxopentanimidic acid
Canonical SMILES CC(CC(/N=C(OCC1=CC=CC=C1)\O)/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(C(CF)=O)CC(OC)=O)CC2=CN=CN2)CCC(OC)=O)C
Formula C32H43FN6O10 M.Wt 690.72
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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].

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.