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Caspase-3/7 Inhibitor ICaspase-3/7抑制剂

Caspase-3/7 Inhibitor I

产品编号:A1925
规格 单价 库存 订购数量
10mM (in 1mL DMSO) ¥2,600.00 5-10 工作日发货
1mg ¥850.00 现货
5mg ¥2,250.00 现货
10mg ¥3,750.00 现货
25mg ¥6,000.00 5-10 工作日发货

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Sample solution is provided at 25 µL, 10mM.

引用文献

Dang Q, Song W, Xu D, et al. Kaempferol suppresses bladder cancer tumor growth by inhibiting cell proliferation and inducing apoptosis[J]. Molecular carcinogenesis, 2014.

该产品包含在以下化合物库中:

质量控制

相关生物数据

caspase 3/7
Human bladder cancer cells were treated with caspase 3/7 inhibitor 1 (10 μMM) or kaempferol (100 μM) for 48 h; In combination treatment, caspase 3/7 inhibitor 1 was added 1 h prior to kaempferol treatment. At the end of treatment, cell extracts were prepared for caspase-7 activity assay. Error bars represent SEs. *P < 0.05.

化学结构

Caspase-3/7 Inhibitor I

Caspase-3/7 Inhibitor I Dilution Calculator

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化学性质

CAS号 220509-74-0 SDF Download SDF
化学名 5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl-1H-indole-2,3-dione
SMILES COCC1CCCN1S(=O)(=O)C2=CC3=C(C=C2)NC(=O)C3=O
分子式 C14H16N2O5S 分子量 324.4
溶解性 >16.2mg/mL in DMSO 储存条件 Store at -20°C
运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

Caspase-3/7 Inhibitor I是一种有效的、细胞通透性的、特异性的和可逆的caspase-3和caspase-7抑制剂,Ki值分别为60 nM和170 nM。.
靶点 Caspase-3 Caspase-7        
Ki 60nM 170nM        

实验操作

细胞实验[1]:

细胞系

人Jurkat T细胞

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

50 μM

应用

用喜树碱(camptothecin)处理细胞可诱导细胞死亡。用FACS分析对Caspase-3/7 Inhibitor I抑制细胞死亡的能力进行评估。Caspase-3/7 Inhibitor I基于细胞的活性与其体外对分离caspase 3或7的抑制活性具有良好的相关性。Caspase-3/7 Inhibitor I在50 μM时抑制54%的细胞凋亡,在10 μM时抑制22%的细胞凋亡。

动物实验:

动物模型

剂量

应用

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Lee D, Long S A, Murray J H, et al. Potent and selective nonpeptide inhibitors of caspases 3 and 7. Journal of medicinal chemistry, 2001, 44(12): 2015-2026.

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研究更新

1. Tissue inhibitor of metalloproteinases-3 moderates the proinflammatory status of macrophages. Am J Respir Cell Mol Biol. 2013 Nov;49(5):768-77. doi: 10.1165/rcmb.2012-0377OC.
Abstract
TIMP-3 is involved in the regulation of inflammation where, in the absence of TIMP3, macrophages are more likely to be differentiated into proinflammatory (M1) cells.
2. [X-linked inhibitor of apoptosis protein (XIAP) and Survivin suppression on human pancreatic cancer cells Panc-1 proliferation and chemosensitivety]. Beijing Da Xue Xue Bao. 2013 Apr 18;45(2):242-9.
Abstract
The effects of inhibition of XIAP, Survivin or both on cell proliferation and chemosensitivity of Panc-1 cells have been investigated and compared.
3. [Effect of aurora kinase B inhibitor AZD1152 in the treatment of cisplatin-resistant ovarian carcinoma]. Zhonghua Fu Chan Ke Za Zhi. 2013 Jan;48(1):46-50.
Abstract
The effect of AZD1152 alone or in combination with cisplatin has been investigated in the treatment of cisplatin-resistant ovarian carcinoma.
4. Targeting X-linked inhibitor of apoptosis protein inhibits pancreatic cancer cell growth through p-Akt depletion. World J Gastroenterol. 2012 Jun 21;18(23):2956-65. doi: 10.3748/wjg.v18.i23.2956.
Abstract
The regulation of XIAP gene by lentivirus-mediated shRNA has been investigated for its effect in the treatment of pancreatic cancer.

产品描述

Caspase-3/7 inbibitor I是一种有效的、可逆的靛红磺酰胺类caspase-3和caspase-7抑制剂,Ki值分别为60 nM和170 nM,对caspase-9具有较弱的作用,Ki值为3.1 mM,而对caspase-1、caspase-2、caspase-4、caspase-6和caspase-8几乎不起作用(Ki>25 mM)。在喜树碱(camptothecin)处理的Jurkat细胞中,Caspase-3/7 inbibitor I抑制细胞凋亡,IC50值约为50 μM。在软骨细胞中,Caspase-3/7 inbibitor I也可以抑制细胞凋亡(10 μM时抑制44%的细胞凋亡,50 μM时抑制98%的细胞凋亡)[1] [2]。抑制caspases-3和caspase-7的活性可以抑制细胞凋亡,因而可能具有重要的治疗意义[3]。

参考文献:
1.  Lee, D., et al. 2001. J. Med. Chem. 44, 2015.
2.  Lee, D., et al. 2000. J. Biol. Chem. 275, 16007.
3.  Clements, K. M., Burton‐Wurster, N., Nuttall, M. E., & Lust, G. (2005). Caspase‐3/7 inhibition alters cell morphology in mitomycin‐c treated chondrocytes. Journal of cellular physiology, 205(1), 133-140.