Caspase-3/7 Inhibitor I
目录号 : GC11718
An isatin sulfonamide-based inhibitor of caspase-3 and caspase-7
Cas No.:220509-74-0
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment: [1] | |
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Cell lines |
Human Jurkat T cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
50 μM |
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Applications |
Cells were treated with camptothecin to induce cell death, and the ability of the compound to inhibit cell death was assessed by FACS analysis. A good correlation exists between relative cell-based activities of the compound with its in vitro isolated caspase 3 or 7 inhibition activites. The compound exhibited 54% inhibition of apoptosis at 50 μM and 22% at 10 μM. |
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Animal models |
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Dosage form |
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Applications |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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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| Cas No. | 220509-74-0 | SDF | |
| 化学名 | 5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl-1H-indole-2,3-dione | ||
| Canonical SMILES | COCC1CCCN1S(=O)(=O)C2=CC3=C(C=C2)NC(=O)C3=O | ||
| 分子式 | C14H16N2O5S | 分子量 | 324.4 |
| 溶解度 | ≥ 16.2mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0826 mL | 15.4131 mL | 30.8261 mL |
| 5 mM | 0.6165 mL | 3.0826 mL | 6.1652 mL |
| 10 mM | 0.3083 mL | 1.5413 mL | 3.0826 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet