Novel polypeptide that suppresses neuronal cell death induced by several familial Alzheimer’s disease genes and by amyloid beta-protein (human). The secretion of amyloid beta-protein (1-40) and amyloid beta protein (1-42) has been shown not to be affected by humanin in F11 cells expressing the familial Alzheimer’s disease gene K595N/M596L-APP. Inhibitory actions on neuronal cell death triggered by K595N/M596L-APP directly and caused by amyloid beta-protein have been suggested.
溶解度
分子量
475.6
化学式
C26H41N3O5
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
Ac-DEVD-CHO is a specific Caspase-3 inhibitor with a Ki value of 230 pM.
IC50 & Target[1]
Caspase-1
18 nM (Ki)
Caspase-2
1710 nM (Ki)
Caspase 3
0.23 nM (Ki)
Caspase-4
132 nM (Ki)
Caspase-5
205 nM (Ki)
Caspase-6
31 nM (Ki)
Caspase-7
1.6 nM (Ki)
Caspase-8
0.92 nM (Ki)
Caspase-9
60 nM (Ki)
Caspase-10
12 nM (Ki)
体外研究 (In Vitro)
To ascertain the role of caspase-3 in SLNT-induced apoptosis, a caspase-3 inhibitor (Ac-DEVD-CHO) is used. The addition of Ac-DEVD-CHO significantly prevents SLNT-induced apoptosis (from 32.91±1.21% decreases to 15.88±1.58% while NC and Ac-DEVD-CHO groups are 6.45±0.96%, 7.77±0.79%, respectively)[2]. The apoptosis rates of cells pretreated with zVAD-fmk (5.32%) or Ac-DEVD-CHO (7.43%) decrease obviously after hypericin-mediated PDT treatment[3]. Remarkably, 10 μmol/L Ac-DEVD-CHO partially blocks the effect of SIN-induced apoptosis and reduces 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, increases caspase-3 activity, which is also blocked by Ac-DEVD-CHO[4].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (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 restored 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 are 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: 1033.2±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 rates 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)%[5].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
502.47
Formula
C20H30N4O11
CAS 号
169332-60-9
Sequence
N-Acetyl-Asp-Glu-Val-Asp-al
Sequence Shortening
Ac-DEVD-al
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Garcia-Calvo M, et al.nhibition of human caspases by peptide-based and macromolecular inhibitors. J Biol Chem. 1998 Dec 4;273(49):32608-13.
[2]. Jinglin Wang, et al. A polysaccharide from Lentinus edodes inhibits human colon cancer cell proliferation and suppresses tumor growth in athymic nude mice. Oncotarget. 2017 Jan 3; 8(1): 610-623.
[3]. Junping Zhang, et al. Hypericin-mediated photodynamic therapy induces apoptosis of myoloma SP2/0 cells depended on caspase activity in vitro. Cancer Cell Int. 2015; 15: 58
[4]. Long-gang He, et al. Sinomenine induces apoptosis in RAW 264.7 cell-derived osteoclasts in vitro via caspase-3 activation. Acta Pharmacol Sin. 2014 Feb; 35(2): 203-210.
[5]. Liu LX, et al. The effect of caspase-3 inhibitor on the concentrations of serum inflammatory cytokines in sepsis related acute kidney injury induced by peritoneal cavity infection in mice. Zhongguo Wei Zhong Bing Ji Jiu Yi Xue. 2010 Dec;22(12):736-9.
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 staineing 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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [5]
One hundred and two male mice are subjected to cecal ligation and puncture 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. The 4-day and 7-day survival rates of three groups of mice are observed[5].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Garcia-Calvo M, et al.nhibition of human caspases by peptide-based and macromolecular inhibitors. J Biol Chem. 1998 Dec 4;273(49):32608-13.
[2]. Jinglin Wang, et al. A polysaccharide from Lentinus edodes inhibits human colon cancer cell proliferation and suppresses tumor growth in athymic nude mice. Oncotarget. 2017 Jan 3; 8(1): 610-623.
[3]. Junping Zhang, et al. Hypericin-mediated photodynamic therapy induces apoptosis of myoloma SP2/0 cells depended on caspase activity in vitro. Cancer Cell Int. 2015; 15: 58
[4]. Long-gang He, et al. Sinomenine induces apoptosis in RAW 264.7 cell-derived osteoclasts in vitro via caspase-3 activation. Acta Pharmacol Sin. 2014 Feb; 35(2): 203-210.
[5]. Liu LX, et al. The effect of caspase-3 inhibitor on the concentrations of serum inflammatory cytokines in sepsis related acute kidney injury induced by peritoneal cavity infection in mice. Zhongguo Wei Zhong Bing Ji Jiu Yi Xue. 2010 Dec;22(12):736-9.
Aldeyde PEG is an amine reactive PEG derivative that can be used to modify biomolecules via available amine groups. The reaction between aldehyde group with ε-amine of lysine residues and the α-amine at the N-terminus produces an intermediate Schiff base. Further reduction with hydride will form a stable C-N bond. PEG aldehydes react with amine groups at a pH of from 5.5 to 9.5. Higher pH will result in multiple Pegylation with both terminal and lysine groups. Aldehyde PEG is a commonly used PEG reagent for n-terminus pegylation in proteins or peptides.
Aldeyde PEG is an amine reactive PEG derivative that can be used to modify biomolecules via available amine groups. The reaction between aldehyde group with ε-amine of lysine residues and the α-amine at the N-terminus produces an intermediate Schiff base. Further reduction with hydride will form a stable C-N bond. PEG aldehydes react with amine groups at a pH of from 5.5 to 9.5. Higher pH will result in multiple Pegylation with both terminal and lysine groups. Aldehyde PEG is a commonly used PEG reagent for n-terminus pegylation in proteins or peptides.
Peptide aldehyde that corresponds to one of the cleavage sites of the inactive 32 kD caspase-3 precursor (amino acids 25-28). In a concentration range of 2.5-5 碌M, it blocks the formation of the p17 subunit and concomitantly induces the accumulation of the p20 peptide.
溶解度
分子量
533.6
化学式
C20H31N5O10S1
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
This biotinylated apopain inhibitor has successfully been used for the affinity purification, on a streptavidin-agarose column, of caspase-3 (apopain); the enzyme that cleaves the poly(ADP-ribose) polymerase (PARP). This inhibitor showed an inhibitory act
溶解度
分子量
502.5
化学式
C21H34N4O10
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
Z. Han et al, J. Biol Chem., 272, 13422 (1997) M.Garcia-Calvo et al., J. Biol. Chem., 273, 32608 (1998)
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