PAC-1
(Synonyms: Procaspase activating compound 1) 目录号 : GC11993
An in vitro procaspase-3 activator
Cas No.:315183-21-2
Sample solution is provided at 25 µL, 10mM.
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First procaspase-activating compound (PAC-1) is a small-molecule activator of procaspase-3 that directly catalyzes the maturation of procaspase-3 to the active caspase-3 by inducing the cleavage of procaspase-3 in a time-dependent manner. As a result of the direct and immediate activation of procaspase-3, PAC-1 potently induces apoptosis in cancer cell lines. The PAC-1 induced apoptosis has been observed to be proportional to the concentrations of procaspase-3 inside the cells of primary colon cancer isolates. Study results have demonstrated that PAC-1 is able to induce cell death in both primary cancerous cells and adjacent normal tissues with 50% inhibition concentration IC50 values ranging from 0.003 to 1.41 μM and 5.02 to 9.98 μM respectively.
Reference
[1].Putt KS, Chen GW, Pearson JM, Sandhorst JS, Hoagland MS, Kwon JT, Hwang SK, Jin H, Churchwell MI, Cho MH, Doerge DR, Helferich WG, Hergenrother PJ. Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat Chem Biol. 2006 Oct;2(10):543-50. Epub 2006 Aug 27.
| Cell experiment [1]: | |
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Cell lines |
Several cancer cell lines (leukemia, lymphoma, melanoma, neuroblastoma, breast cancer, lung cancer, adrenal cancer and renal cancer) |
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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 |
72 hrs |
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Applications |
PAC-1 induces cell death in a procaspase-3-dependant manner. PAC-1 is most potent against the lung cancer cell line NCI-H226, with an IC50 value of 0.35 μM. |
| Animal experiment [1]: | |
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Animal models |
Mice s.c. injected with NCI-H226 (lung cancer) cells |
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Dosage form |
0, 50 or 100 mg/kg; p.o.; q.d., for 21 days |
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Applications |
In mice s.c. injected with NCI-H226 (lung cancer) cells, PAC-1 significantly retarded tumor growth in a dose-dependent manner. |
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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]. Putt KS, Chen GW, Pearson JM, Sandhorst JS, Hoagland MS, Kwon JT, Hwang SK, Jin H, Churchwell MI, Cho MH, Doerge DR, Helferich WG, Hergenrother PJ. Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat Chem Biol. 2006 Oct;2(10):543-50. Epub 2006 Aug 27. |
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| Cas No. | 315183-21-2 | SDF | |
| 别名 | Procaspase activating compound 1 | ||
| 化学名 | 2-(4-benzylpiperazin-1-yl)-N'-[(Z)-(6-oxo-5-prop-2-enylcyclohexa-2,4-dien-1-ylidene)methyl]acetohydrazide | ||
| Canonical SMILES | C=CCC1=CC=CC(=CNNC(=O)CN2CCN(CC2)CC3=CC=CC=C3)C1=O | ||
| 分子式 | C23H28N4O2 | 分子量 | 392.49 |
| 溶解度 | ≥ 13.4mg/mL in DMSO, ≥ 6.87 mg/mL in EtOH with ultrasonic | 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 | 2.5478 mL | 12.7392 mL | 25.4784 mL |
| 5 mM | 0.5096 mL | 2.5478 mL | 5.0957 mL |
| 10 mM | 0.2548 mL | 1.2739 mL | 2.5478 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