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Ac-DEVD-CHO

Ac-DEVD-CHO用途

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

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Ac-DEVD-CHO名称

[ CAS 号 ]:
169332-60-9

[ 中文名 ]:
乙酰基-天冬氨酰-谷氨酰-缬氨酰-天冬氨醛

[ 英文名 ]:
Ac-DEVD-CHO

[英文别名 ]:

N-Acetyl-Asp-Glu-Val-Asp-al

Ac-DEVD-CHO生物活性

[ 描述 ]:

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

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 胱天蛋白酶

研究领域 >> 癌症

多肽产品

[ 靶点 ]

Caspase 3:0.23 nM (Ki)

Caspase-8:0.92 nM (Ki)

Caspase-7:1.6 nM (Ki)

Caspase-10:12 nM (Ki)

Caspase-1:18 nM (Ki)

Caspase-6:31 nM (Ki)

Caspase-9:60 nM (Ki)

Caspase-4:132 nM (Ki)

Caspase-5:205 nM (Ki)

Caspase-2:1710 nM (Ki)

[体外研究]

为了确定胱天蛋白酶-3在SLNT诱导的细胞凋亡中的作用,使用半胱天冬酶-3抑制剂(Ac-DEVD-CHO)。添加Ac-DEVD-CHO可显着预防SLNT诱导的细胞凋亡(从32.91±1.21％降至15.88±1.58％,而NC和Ac-DEVD-CHO组分别为6.45±0.96％,7.77±0.79％)[2] ]。经金丝桃素介导的PDT处理后,经zVAD-fmk(5.32％)或Ac-DEVD-CHO(7.43％)预处理的细胞凋亡率明显下降[3]。值得注意的是,10μmol/ L Ac-DEVD-CHO部分阻断了SIN诱导的细胞凋亡的作用并减少了凋亡细胞核的数量。 SIN的这些作用被胱天蛋白酶-3抑制剂Ac-DEVD-CHO阻断。喜树碱(4μM)是一种阳性对照,可增加caspase-3活性,这也被Ac-DEVD-CHO阻断[4]。

[体内研究]

与模型组比较,CI组血清BUN浓度在术后各时间点均明显降低,6小时后Cr明显降低,12小时和24小时恢复为假手术组;在所有时间点,血清TNF-α,IL-6浓度均降低,IL-10浓度显着升高。 [TNF-α(μg/ L)6小时：436.2±64.2对比653.6±8.9,12小时：233.4±85.4对比579.7±137.1,24小时：151.0±90.3对比551.0±119.8,IL-6(μg)/L)6小时：1033.2±345.8对比1 595.3±159.4,12小时：366.3±68.3对比1 330.7±249.8,24小时：241.2±208.4对比815.3±572.7,IL-10(μg/ L)6小时：33.6±10.4对比26.6±4.5,12小时：37.2±5.0对比24.5±4.3,24小时：38.3±5.5对比18.2±1.6,所有P <0.05];肾细胞凋亡率在所有时间点均显着下降：凋亡率为6小时：(13.9±3.2)％对比(18.3±1.4)％,12小时：(10.5±3.6)％对比(15.9±3.5)％ ,24小时：(8.4±1.8)％vs.(12.5±2.1)％[5]。

[细胞实验]

将OCL与RANKL一起温育，并用含有或不含特异性半胱天冬酶-3抑制剂Ac-DEVD-CHO（10μM）的0.5mM SIN处理24小时。在处理结束时，用PBS洗涤细胞，并用10μMHoechst33258染料染色15分钟。用荧光显微镜捕获staineing细胞的图像。通过计数每个孔中具有凋亡核浓缩的细胞数来评估差异[4]。

[动物实验]

对102只雄性小鼠进行盲肠结扎和穿刺或假手术。根据随机数表将动物分成三个相等的组（n = 34）：假手术组，模型组和半胱天冬酶-3抑制剂（CI）组。在CLP前30分钟，在CI组中皮下注射Ac-DEVD-CHO（4μg/ g）。测定血尿素氮（BUN）和肌酐（Cr）水平，用酶联免疫吸附试验测定肿瘤坏死因子-α（TNF-α），白细胞介素（IL-6和IL-10）的浓度（ ELISA），通过流式细胞术测定肾细胞凋亡率。观察三组小鼠的4天和7天存活率[5]。

[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.

[相关活性小分子]

Ac-DEVD-CHO物理化学性质

[ 密度 ]:
1.374g/cm3

[ 沸点 ]:
1021.1ºC at 760mmHg

[ 分子式 ]:
C₂₀H₃₀N₄O₁₁

[ 分子量 ]:
502.47200

[ 闪点 ]:
571.3ºC

[ 精确质量 ]:
502.19100

[ PSA ]:
245.37000

[ 蒸汽压 ]:
0mmHg at 25°C

[ 折射率 ]:
1.535

[ 储存条件 ]:
-20°C

Ac-DEVD-CHOMSDS

详细MSDS(安全技术说明书)

Ac-DEVD-CHO安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

Ac-DEVD-CHO文献

The novel HDAC inhibitor AR-42-induced anti-colon cancer cell activity is associated with ceramide production.

Biochem. Biophys. Res. Commun. 463 , 545-50, (2015)

In the current study, we investigated the potential activity of AR-42, a novel histone deacetylase (HDAC) inhibitor, against colon cancer cells. Our in vitro results showed that AR-42 induced ceramide...

Artesunate-enhanced apoptosis of human high-risk myelodysplastic cells induced by the DNA methyltransferase inhibitor decitabine.

Oncol. Lett. 9 , 2449-2454, (2015)

The present study aimed to investigate whether artesunate (ART) could enhance the rate of apoptosis induced by decitabine (DAC) in the high-risk myelodysplastic syndrome (MDS) SKM-1 cell line, and exa...

Synthetic ion transporters can induce apoptosis by facilitating chloride anion transport into cells.

Nature Chemistry 6(10) , 885-92, (2014)

Anion transporters based on small molecules have received attention as therapeutic agents because of their potential to disrupt cellular ion homeostasis. However, a direct correlation between a change...

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