Z-LEHD-FMK TFA

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Z-LEHD-FMK TFA 

Z-LEHD-FMK TFA 是一种选择性和不可逆的 caspase-9 抑制剂，可防止致命的再灌注损伤并减弱细胞凋亡。Z-LEHD-FMK TFA 在大鼠脊髓损伤模型中也表现出神经保护作用。

Z-LEHD-FMK TFA

Z-LEHD-FMK TFA Chemical Structure

CAS No. : 524746-03-0

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Z-LEHD-FMK TFA 的其他形式现货产品:

Z-LEHD-FMK

生物活性

Z-LEHD-FMK TFA is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK TFA exhibits the neuroprotective effect in a rat model of spinal cord trauma[1][2][3].

IC50 & Target

Caspase-9

 

体外研究
(In Vitro)

Z-LEHD-FMK (20 μM; pretreated for 30 min) completely protects HCT116 and 293 cells from TRAIL-induced toxicity[1].
Z-LEHD-FMK (20 μM ; 6 h) protects normal human hepatocytes from TRAIL-induced apoptosis[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: SW480, H460, HCT116 and 293 cells
Concentration: 20 μM
Incubation Time: Pretreated for 30 min
Result: Protected HCT116 and 293 cells from TRAIL-induced apoptosis.

Western Blot Analysis[1]

Cell Line: HCT116, SW480 cells
Concentration: 20 μM
Incubation Time: 2 h
Result: Protected procaspase 3 from cleavage in HCT116 cells but not in SW480 cells, especially at the 16-h time point.

体内研究
(In Vivo)

Z-LEHD-FMK (0.8 μmol/kg; i.v. for 7 d) protects neurons, glia, myelin, axons, and intracellular organelles in spinal cord injury (SCI) rats[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar albino rats (250-350 g) with SCI[2]
Dosage: 0.8 μmol/kg
Administration: I.v. for 1 or 7 days
Result: Decreased the mean apoptotic cell count at 24 hours and 7 days postinjury.

分子量

804.74

Formula

C34H44F4N6O12
CAS 号

524746-03-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

H2O

Peptide Solubility and Storage Guidelines:

1.  Calculate the length of the peptide.

2.  Calculate the overall charge of the entire peptide according to the following table:

  Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.  Recommended solution:

Overall charge of peptide Details
Negative (<0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, add NH4OH (<50 μL).
3.  If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.  If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.  Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.  For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献

  • [1]. Ozoren N, 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 Nov 15; 60(22): 6259-65.

    [2]. Colak A, 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 Mar; 2(3): 327-34.

    [3]. Mocanu MM, et, al. Caspase inhibition and limitation of myocardial infarct size: protection against lethal reperfusion injury. Br J Pharmacol. 2000 May; 130(2): 197-200.

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