PSI
(Synonyms: Z-异亮氨酰-叔丁基谷氨酰-丙氨酸-亮氨酸缩醛,Z-Ile-Glu(OtBu)-Ala-Leu-CHO) 目录号 : GC13865
PSI (Proteasome Inhibitor 1) 是一种有效的蛋白酶体抑制剂。
Cas No.:158442-41-2
Sample solution is provided at 25 µL, 10mM.
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ZIE(OtBu)AL-CHO (PSI)1 have been shown to inhibit the proteasome activities in a variety of cell types.
Peptide aldehyde, PSI (Z-Ile-Glu(OtBu)-Ala-Leu-al), inhibits the proteasome 10-fold better than calpain but is less potent than MG1322. Since MG132, PSI, MG115 (Z-Leu-Leu-nVal-al) and ALLN can all inhibit calpains and various lysosomal cathepsins in addition to the proteasome, when using these inhibitors in cell culture it is important to perform control experiments to con¢rm that the observed e¡ects are due to the inhibition of the proteasome. First, one can use agents, which block intracellular cysteine proteases, but do not inhibit proteasomes3. Such inhibitors are Z-Leu-Leu- al, and E-64 for calpains4, and weak bases such as chloroquine and E-64 for lysosomal proteolysis . In yeast, where digestive vacuoles contain mainly serine, not cysteine, proteases, phenylmethylsulfonyl £uoride can be used to inhibit these enzymes without affecting proteasomes5.
Despite the availability of these inhibitors, MG132, due to its low cost and the rapid reversibility of its action, still remains, in our opinion, the first choice to study proteasome involvement in a process in cell cultures or tissues, if appropriate controls are used. As the most potent and selective of commercially available aldehydes, MG132 is preferable to ALLN, MG115 (Z-Leu-Leu-nVal-al), or even PSI. On the other hand, the least selective inhibitor, ALLN, because of its ability to inhibit most major pro teases in mammalian cells, is probably the best tool for prevention of unwanted proteolysis, for example during isolation of proteins from mammalian cells.
Reference:
1. Takada K (1995) Mol. Biol. Rep. 21: 21–26
2. A. F. Kisselev, A. L. Goldberg. Proteasome inhibitors: from research tools to drug candidates. Chemistry & Biology 8 (2001) 739-758.
3. W. Matthews, J. Driscoll, K. Tanaka, A. Ichihara, A.L. Goldberg, Involvement of the proteasome in various degradative processes in mammalian cells, Proc. Natl. Acad. Sci. USA 86 (1989) 2597-2601.
4. S. Tsubuki, Y. Saito, M. Tomioka, H. Ito, S. Kawashima, Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine, J. Biochem. 119 (1996) 572-576.
5. D.H. Lee, A.L. Goldberg, Selective inhibitors of the proteasome-dependent and vacuolar pathways of protein degradation in Saccharomyces cerevisiae, J. Biol. Chem. 271 (1996) 27280-27284.
| Cell experiment: [1] | |
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Cell lines |
STAV-AB and STAV-FCS 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 |
IC50: 4.01μM for STAV-AB, 24 hours 16.31μM for STAV-FCS, 24 hours |
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Applications |
Treatment with PSI reduced the viability of the two MM cell sub-lines to different extents in a time and concentration-dependent manner. Thus exposure to PSI for 24 h resulted in an IC50of 4.01μM on STAV-AB cells, but 16.31μM of the same drug was needed for a similar reduction in cell numbers on STAV-FCS cells. |
| Animal experiment: [2] | |
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Animal models |
Male Sprague-Dawley adult rats |
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Dosage form |
Subcutaneous injection, 6.0 mg/kg |
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Applications |
The effects of PSI treatment on the amount of dopamine and the dopamine metabolite DOPAC in the striata, were evaluated by HPLC analysis. Decreased levels of DA in the striatum were found at 6 weeks after the end of PSI treatment as compared to controls; a decrement was also observed in the level of DOPAC in the PSI-treated rats, but did not reach statistical significance. DOPAC/DA ratio was unchanged in the PSI-treated rats as compared to controls, highlighting that reduction of DA level in the striatum of PSI treated rats was not attributable to increased DA metabolism. |
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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] Sun X, Gulyás M, Hjerpe A, et al. Proteasome inhibitor PSI induces apoptosis in human mesothelioma cells. Cancer letters, 2006, 232(2): 161-169. [2] Pizzi S D, Rossi C, Di Matteo V, et al. Morphological and metabolic changes in the nigro-striatal pathway of synthetic proteasome inhibitor (PSI)-treated rats: a MRI and MRS study. PloS one, 2013, 8(2): e56501. | |
| Cas No. | 158442-41-2 | SDF | |
| 别名 | Z-异亮氨酰-叔丁基谷氨酰-丙氨酸-亮氨酸缩醛,Z-Ile-Glu(OtBu)-Ala-Leu-CHO | ||
| 化学名 | tert-butyl (4S)-5-[[(2S)-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-[[(2S,3R)-3-methyl-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-5-oxopentanoate | ||
| Canonical SMILES | CCC(C)C(C(=O)NC(CCC(=O)OC(C)(C)C)C(=O)NC(C)C(=O)NC(CC(C)C)C=O)NC(=O)OCC1=CC=CC=C1 | ||
| 分子式 | C32H50N4O8 | 分子量 | 618.76 |
| 溶解度 | ≥ 30.6mg/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 | 1.6161 mL | 8.0807 mL | 16.1614 mL |
| 5 mM | 0.3232 mL | 1.6161 mL | 3.2323 mL |
| 10 mM | 0.1616 mL | 0.8081 mL | 1.6161 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