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Caspase-3/7 Inhibitor I

Catalog No.
A1925
Caspase-3/7抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,600.00
现货
1mg
¥ 850.00
现货
5mg
¥ 2,250.00
现货
10mg
¥ 3,750.00
现货
25mg
¥ 6,000.00
现货

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Background

Caspase-3/7 inbibitor I is a potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (KI(app) = 60 nM) and caspase-7 (KI(app) = 170 nM). Is a weaker inhibitor of caspase-9 (Ki(app) = 3.1 mM). It Has only a trivial effect (Ki(app) >25 mM) on the activities of caspase-1, caspase-2, caspase-4, caspase-6, and caspase-8. It has been shown to inhibit apoptosis in camptothecin treated Jurkat cells (IC50 ~50 µM). Also it has been reported to inhibit apoptosis in chondrocytes (44% inhibition at 10 µM and 98% inhibition at 50 µM). Selectivity for caspases-3 and 7 involves unique hydrophobic residues in the S2 pocket surrounding the catalytic cysteine residue. [1] [2] In some systems inhibition of caspases-3 and -7 can prevent apoptosis and may therefore have important therapeutic implications. [3]

A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (Ki = 60 nM) and caspase-7 (Ki = 170 nM).

References:
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.

文献引用

1.DXie L, Dai H, et al. "MARCH1 encourages tumour progression of hepatocellular carcinoma via regulation of PI3K-AKT-β-catenin pathways." J Cell Mol Med. 2019 May;23(5):3386-3401. PMID:30793486
2.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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt324.4
Cas No.220509-74-0
FormulaC14H16N2O5S
Solubility≥16.2mg/mL in DMSO
Chemical Name5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl-1H-indole-2,3-dione
SDFDownload SDF
Canonical SMILESCOCC1CCCN1S(=O)(=O)C2=CC3=C(C=C2)NC(=O)C3=O
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。

试验操作

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.

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        

质量控制

化学结构

Caspase-3/7 Inhibitor I

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.

相关生物数据

Caspase-3/7 Inhibitor I