PI-1840
Based on 1 Customer Validation
PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.78%
- CAS 番号: 1401223-22-0
- 分子式: C22H26N4O3
- 分子量:394.47
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
2.95 nM
Compound: 6; PI-1840
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Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
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[PMID: 30391816] |
| HGC-27 | IC50 |
3.35 nM
Compound: 6; PI-1840
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Antiproliferative activity against human HGC27 cells after 72 hrs by MTT assay
Antiproliferative activity against human HGC27 cells after 72 hrs by MTT assay
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[PMID: 30391816] |
| MDA-MB-231 | IC50 |
7.6 μM
Compound: PI-1840
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Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by SRB assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by SRB assay
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[PMID: 32853683] |
| MM1.S | IC50 |
>20 nM
Compound: 6; PI-1840
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Antiproliferative activity against human MM1S cells after 72 hrs by MTS/PMS assay
Antiproliferative activity against human MM1S cells after 72 hrs by MTS/PMS assay
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[PMID: 30391816] |
| MV4-11 | IC50 |
>20 nM
Compound: 6; PI-1840
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Antiproliferative activity against human MV4-11 cells after 72 hrs by MTS/PMS assay
Antiproliferative activity against human MV4-11 cells after 72 hrs by MTS/PMS assay
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[PMID: 30391816] |
| RPMI-8226 | IC50 |
>20 nM
Compound: 6; PI-1840
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Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS/PMS assay
Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS/PMS assay
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[PMID: 30391816] |
体外実験
PI-1840 (5-60 µM; 24 and 48 h) inhibits the proliferation of MG-63 and U2-OS cells[1].
PI-1840 (40 µM (U2-OS cells) and 60 µM (MG-63 cells); 24 and 48 h) induces cell cycle arrest at the G2/M phase[1].
PI-1840 (15-60 µM (MG-63 cells), 10-40 µM (U2-OS cells); 48 h) induces apoptosis through NF-κB pathway in MG-63 and U2-OS cells. PI-1840 induces autophagy in MG-63 and U2-OS cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MG-63 and U2-OS cells
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Concentration:5, 10, 20, 40, 80, and 160 µM
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Incubation Time:24 and 48 hours
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Result:Inhibited cell growth in a dose-dependent manner with IC50 values of 108.40 µM (MG-63, 24 h), 59.58 µM (MG-63, 48 h), 86.43 µM (U2-OS, 24 h), and 38.83 µM (U2-OS, 48 h), respectively.
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Cell Line:MG-63 and U2-OS cells
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Concentration:15, 30, and 60 µM (MG-63 cells), 10, 20, and 40 µM (U2-OS cells)
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Incubation Time:48 hours
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Result:Increased the apoptotic rates of the two cell lines in a dose-dependent manner.
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Cell Line:MG-63 and U2-OS cells
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Concentration:40 µM (U2-OS cells) and 60 µM (MG-63 cells)
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Incubation Time:24 and 48 hours
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Result:Increased in the G2/M phase cell population.
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Cell Line:MG-63 and U2-OS cells
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Concentration:40 µM (U2-OS cells) and 60 µM (MG-63 cells)
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Incubation Time:24 and 48 hours
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Result:Increased the cell cycle regulation-associated proteins about p21, p27 and WEE1.
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Cell Line:MG-63 and U2-OS cells
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Concentration:15, 30, and 60 µM (MG-63 cells), 10, 20, and 40 µM (U2-OS cells)
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Incubation Time:48 hours
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Result:Increased the ratio of the expression level of (p-IκBα/control)/(IκBα/control), and decreased the ratio of (p-p65/control)/(p65/control).
Decreased the expression level of Bcl-2 and the mitochondrial proteins Cyto c.
Increased the expression levels of Bax, and the ratios of (cleaved caspase-3/caspase-3, cleaved PARP/PARP, cleaved caspase-8/caspase-8 and cleaved caspase-9/caspase-9.
Increased the ratio of LC3 II to LC 3 I, and the expression level of Beclin1.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice with MDA-MB-231 xenografts[2]
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Dosage:150 mg/kg
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Administration:Intraperitoneal injection; daily, for 14 days
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Result:Inhibited the growth of MDA-MB-231 tumor xenografts by 76%.
化学情報
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CAS 番号 1401223-22-0
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性状 Solid
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分子量 394.47
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分子式 C22H26N4O3
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Color White to off-white
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SMILES
O=C(N(C(C)C)CC1=NC(C2=CC=CN=C2)=NO1)COC3=CC=C(CCC)C=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (253.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kazi A, et, al. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. J Biol Chem. 2014 Apr 25;289(17):11906-11915. [Content Brief]
[2]. Chen Y, et, al. Non covalent proteasome inhibitor PI 1840 induces apoptosis and autophagy in osteosarcoma cells. Oncol Rep. 2019 May;41(5):2803-2817. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5350 mL | 12.6752 mL | 25.3505 mL | 63.3762 mL |
| 5 mM | 0.5070 mL | 2.5350 mL | 5.0701 mL | 12.6752 mL | |
| 10 mM | 0.2535 mL | 1.2675 mL | 2.5350 mL | 6.3376 mL | |
| 15 mM | 0.1690 mL | 0.8450 mL | 1.6900 mL | 4.2251 mL | |
| 20 mM | 0.1268 mL | 0.6338 mL | 1.2675 mL | 3.1688 mL | |
| 25 mM | 0.1014 mL | 0.5070 mL | 1.0140 mL | 2.5350 mL | |
| 30 mM | 0.0845 mL | 0.4225 mL | 0.8450 mL | 2.1125 mL | |
| 40 mM | 0.0634 mL | 0.3169 mL | 0.6338 mL | 1.5844 mL | |
| 50 mM | 0.0507 mL | 0.2535 mL | 0.5070 mL | 1.2675 mL | |
| 60 mM | 0.0423 mL | 0.2113 mL | 0.4225 mL | 1.0563 mL | |
| 80 mM | 0.0317 mL | 0.1584 mL | 0.3169 mL | 0.7922 mL | |
| 100 mM | 0.0254 mL | 0.1268 mL | 0.2535 mL | 0.6338 mL |
PI-1840 関連分類
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