1. Apoptosis
  2. Caspase

Ac-DEVD-CHO (Synonyms: N-Acetyl-Asp-Glu-Val-Asp-al)

目录号: HY-P1001
产品使用指南

Ac-DEVD-CHO 是一种特异性 caspase-3 抑制剂,Ki 为 230 pM.

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Ac-DEVD-CHO Chemical Structure

Ac-DEVD-CHO Chemical Structure

CAS No. : 169332-60-9

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Description

Ac-DEVD-CHO is a specific caspase-3 inhibitor with Ki of 230 pM.

IC50 & Target

Ki: 230 pM (caspase-3)[1].

In Vitro

To ascertain the role of caspase-3 in SLNT-induced apoptosis, a caspase-3 inhibitor (Ac-DEVD-CHO) is used. HT-29 cells are pre-incubated with Ac-DEVD-CHO (25 μM) for 1 h before the addition of SLNT (800 μg/mL). The addition of Ac-DEVD-CHO significantly prevent SLNT-induced apoptosis (from 32.91±1.21% decreased to 15.88±1.58% while NC and Ac-DEVD-CHO group are 6.45±0.96%, 7.77±0.79%, respectively)[2]. To investigate whether apoptosis induced by hypericin-mediated PDT dependent on the activation of capases, SP2/0 cells are pretreated with the 100 μM pan-caspase inhibitor (Z-VAD-FMK) or 100 μM caspase-3 inhibitor (Ac-DEVD-CHO) for 1 h. The apoptosis rate of cells pretreate with zVAD-fmk (5.32%) or Ac-DEVD-CHO (7.43%) decrease obviously after hypericin- mediate PDT treatment[3].Remarkably, 10 μmol/L Ac-DEVD-CHO partially block the effect of SIN-induced apoptosis and reduce the number of apoptotic nuclei. These effects of SIN are blocked by the caspase-3 inhibitor Ac-DEVD-CHO. Camptothecin (4 μM), a positive control, increase caspase-3 activity, which is also blocked by Ac-DEVD-CHO [4].

In Vivo

Compare with model group, in CI group, the concentrations of serum BUN are decreased significantly at all time points after operation and those of Cr are decreased significantly at 6 hours, then restore to those of the sham group at 12 hours and 24 hours; the concentrations of serum TNF-α, IL-6 are decreased and those of IL-10 elevated significantly at all time points [TNF-α (μg/L) 6 hours: 436.2±64.2 vs. 653.6±8.9, 12 hours: 233.4±85.4 vs. 579.7±137.1, 24 hours: 151.0±90.3 vs. 551.0±119.8; IL-6 (μg/L) 6 hours: 1 033.2±345.8 vs. 1 595.3±159.4, 12 hours : 366.3±68.3 vs. 1 330.7±249.8, 24 hours: 241.2±208.4 vs. 815.3±572.7; IL-10 (μg/L) 6 hours : 33.6±10.4 vs. 26.6±4.5, 12 hours: 37.2±5.0 vs. 24.5±4.3, 24 hours: 38.3±5.5 vs. 18.2±1.6, all P<0.05]; the renal cell apoptosis rate and the expression of caspase-3 mRNA are decreased significantly at all time points [apoptosis rates 6 hours: (13.9±3.2)% vs. (18.3±1.4)%, 12 hours: (10.5±3.6)% vs. (15.9±3.5)%, 24 hours: (8.4±1.8)% vs. (12.5±2.1)%; caspase-3 mRNA 6 hours: 1.95±0.16 vs. 3.84±0.35, 12 hours: 1.89±0.19 vs. 3.97±0.73, 24 hours : 2.01±0.20 vs. 4.97±0.24, all P<0.05]. The 4-day survival rate of CI group is improved (80% vs. 20%)[5].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.9902 mL 9.9508 mL 19.9017 mL
5 mM 0.3980 mL 1.9902 mL 3.9803 mL
10 mM 0.1990 mL 0.9951 mL 1.9902 mL
Cell Assay
[4]

OCLs are incubated with RANKL and treated with 0.5 mM SIN with or without the specific caspase-3 inhibitor Ac-DEVD-CHO (10 μM) for 24 h. At the end of the treatment, the cells are washed with PBS and are stained for 15 min with 10 μM Hoechst 33258 dye. Images of the stained cells are captured with a fluorescent microscope. The differences are evaluated by counting the number of cells with apoptotic nuclear condensation in each well[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[5]

One hundred and two male C57BL/6 mice are subjected to cecal ligation and puncture (CLP, a model of polymicrobial sepsis) or sham operation. The animals are assigned into three equal groups (n=34) according to random number table: sham group, model group, and caspase-3 inhibitor (CI) group. Thirty minutes before CLP, Ac-DEVD-CHO (4 μg/g) is injected subcutaneously in CI group. The levels of blood urea nitrogen (BUN) and creatinine (Cr) are determined, and the concentrations of tumor necrosis factor-α (TNF-α), interleukins (IL-6 and IL-10) are measured by enzyme linked immunosorbent assay (ELISA), the renal cell apoptosis rate is determined by flow cytometry and the expression of caspase-3 mRNA is determined by real time reverse transcription-polymerase chain reaction (RT-PCR) at 6, 12 and 24 hours after operation. The 4-day and 7-day survival rates of three groups of mice are observed[5]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

502.47

Formula

C₂₀H₃₀N₄O₁₁

CAS No.

169332-60-9

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Ac-DEVD-CHO
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HY-P1001
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