PU141
Based on 1 Customer Validation
PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.96%
- CAS 番号: 168334-34-7
- 分子式: C14H9F3N2OS
- 分子量:310.29
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Epigenetics Compound Library
HY-L005
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Anti-Pulmonary Fibrosis Compound Library
HY-L125
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
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Lactylation Compound Library
HY-L249
生物活性
CBP/p300[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | GI50 |
4.12 μM
Compound: 2, PU141
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Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTS assay
Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTS assay
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10.1039/C4MD00245H |
| HL-60 | GI50 |
4.12 μM
Compound: 68
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Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CellTiter 96 Aqueous non-radioactive cell proliferation assay
Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CellTiter 96 Aqueous non-radioactive cell proliferation assay
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[PMID: 33045661] |
| LNCaP | GI50 |
36.9 μM
Compound: 2, PU141
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Cytotoxicity against human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay
Cytotoxicity against human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay
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10.1039/C4MD00245H |
| MCF7 | GI50 |
30.2 μM
Compound: 8h
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Growth inhibition of human MCF7 cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay
Growth inhibition of human MCF7 cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay
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[PMID: 21353783] |
| SK-N-SH | GI50 |
0.48 μM
Compound: 8h
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Growth inhibition of human SK-N-SH cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay
Growth inhibition of human SK-N-SH cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay
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[PMID: 21353783] |
PU141 inhibits cell growth at micromolar concentrations in A431 (epidemoid carcinoma), A549 (alveolar basal epithelial adenocarcinoma), A2780 (ovarian carcinoma), HCT116 (epithelial colon carcinoma), HepG2 (hepatocellular carcinoma), MCF7 (breast carcinoma), SK-N-SH (neuroblastoma), SW480 (colon adenocarcinoma) and U-87MG (epithelial-like glioblastoma-astrocytoma)[1].
PU141 causes both histone hypoacetylation and growth inhibition in vitro. PU141 (25 µM) leads to a decrease in SAHA-induced H3K14 and H4K8 hyperacetylation, whereas H3K9 and H4K16 acetylation levels remaine stable after co-treatment of HDAC and HAT inhibitor. The impact on histone acetylation is similar in both SK-N-SH and HCT116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A431 (epidemoid carcinoma), A549 (alveolar basal epithelial adenocarcinoma), A2780 (ovarian carcinoma), HCT116 (epithelial colon carcinoma), HepG2 (hepatocellular carcinoma), MCF7 (breast carcinoma), SK-N-SH (neuroblastoma), SW480 (colon adenocarcinoma) and U-87MG (epithelial-like glioblastoma-astrocytoma)
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Concentration:0, 10, 20, 30, 40, 50, and 60 µM
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Incubation Time:
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Result:Inhibited cell growth at micromolar concentrations in all screened cell lines. The highest cellular antiproliferative activity was detected for the neuroblastoma SK-N-SH cell line.
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Cell Line:SK-N-SH neuroblastoma and HCT116 colon carcinoma cells
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Concentration:25 µM
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Incubation Time:3 hours
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Result:Led to a decrease in SAHA-induced H3K14 and H4K8 hyperacetylation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NMRI:nu/nu mice bearing a xenograft model[1]
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Dosage:12.5 and 25 mg/kg
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Administration:Administered once intraperitoneally (i.p.) as a detergent containing saline microemulsion; for 24 days
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Result:Led to significant tumor volume reduction (19%) at 25 mg/kg.
化学情報
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CAS 番号 168334-34-7
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性状 Solid
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分子量 310.29
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分子式 C14H9F3N2OS
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Color White to off-white
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SMILES
O=C1N(SC2=NC=CC=C21)CC3=CC=C(C=C3)C(F)(F)F
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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 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (322.28 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: 5 mg/mL (16.11 mM); Clear solution; Need ultrasonic and warming and heat to 80°C
This protocol yields a clear solution of 5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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 (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2228 mL | 16.1140 mL | 32.2279 mL | 80.5698 mL |
| 5 mM | 0.6446 mL | 3.2228 mL | 6.4456 mL | 16.1140 mL | |
| 10 mM | 0.3223 mL | 1.6114 mL | 3.2228 mL | 8.0570 mL | |
| 15 mM | 0.2149 mL | 1.0743 mL | 2.1485 mL | 5.3713 mL | |
| 20 mM | 0.1611 mL | 0.8057 mL | 1.6114 mL | 4.0285 mL | |
| 25 mM | 0.1289 mL | 0.6446 mL | 1.2891 mL | 3.2228 mL | |
| 30 mM | 0.1074 mL | 0.5371 mL | 1.0743 mL | 2.6857 mL | |
| 40 mM | 0.0806 mL | 0.4028 mL | 0.8057 mL | 2.0142 mL | |
| 50 mM | 0.0645 mL | 0.3223 mL | 0.6446 mL | 1.6114 mL | |
| 60 mM | 0.0537 mL | 0.2686 mL | 0.5371 mL | 1.3428 mL | |
| 80 mM | 0.0403 mL | 0.2014 mL | 0.4028 mL | 1.0071 mL | |
| 100 mM | 0.0322 mL | 0.1611 mL | 0.3223 mL | 0.8057 mL |
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