HLI373 dihydrochloride
Based on 1 Customer Validation
HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
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- 純度: 98.5%
- CAS 番号: 1782531-99-0
- 分子式: C18H25Cl2N5O2
- 分子量:414.33
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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
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Plasmodium |
HLI373 (3-15 μM; 15 hours) selectively kills tumor cells harboring wild type p53[1].
HLI373 (10-50 μM) stabilizes cellular Hdm2 in a dose-dependent manner.
HLI373 (3 μM) activates p53 transcription[1].
HLI373 selectively inhibits auto-ubiquitylation of Hdm2[1].
Co-transfection with plasmids encoding p53 and Hdm2 results in degradation of p53. Incubation with HLI373 (5-10 μM; 8 hours) blocks p53 degradation. HLI373 increases p53 and Hdm2 protein levels in cells[1].
HLI 373 also shows lower IC50 values (below 6 μM) against both chloroquine-sensitive P. falciparum D6 strain (PfD6) and chloroquine-resistant P. falciparum W2 strain (PfW2) and exhibits early growth inhibition[2].
HLI-373 is a MDM2 inhibitor interrupting its ubiquitin E3 ligase activity, could abolish the ubiquitylation of its substrate protein p53. HLI-373 targets the C-terminus functioning as an E3 ubiquitin ligase[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Wild type p53 mouse embryo fibroblasts (MEFs), and p53-deficient MEFs
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Concentration:3, 10, 15 μM
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Incubation Time:15 hours
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Result:Increased cell death in wild type p53 MEFs in a dose-dependent manner, p53-deficient MEFs were relatively resistant.
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Cell Line:U2OS cells
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Concentration:5, 10 μM
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Incubation Time:8 hours
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Result:Blocked p53 degradation caused by co-transfection with plasmids encoding p53 and Hdm2.
化学情報
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CAS 番号 1782531-99-0
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性状 Solid
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分子量 414.33
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分子式 C18H25Cl2N5O2
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Color Light yellow to yellow
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SMILES
O=C1N=C2N(C)C3=C(C=CC=C3)C(NCCCN(C)C)=C2C(N1C)=O.[H]Cl.[H]Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
H2O : 38 mg/mL (91.71 mM; Need ultrasonic and warming)
DMSO : 4 mg/mL (9.65 mM; Need ultrasonic and warming; 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
[1]. Jirouta Kitagaki, et al. Targeting Tumor Cells Expressing p53 With a Water-Soluble Inhibitor of Hdm2. Mol Cancer Ther. 2008 Aug;7(8):2445-54. [Content Brief]
[2]. Jagrati Jain, et al. Inhibitors of Ubiquitin E3 Ligase as Potential New Antimalarial Drug Leads. BMC Pharmacol Toxicol. 2017 Jun 2;18(1):40. [Content Brief]
[3]. Ying Chen, et al. MDM2 Promotes Epithelial-Mesenchymal Transition and Metastasis of Ovarian Cancer SKOV3 Cells. Br J Cancer. 2017 Oct 10;117(8):1192-1201. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 / H2O | 1 mM | 2.4135 mL | 12.0677 mL | 24.1354 mL | 60.3384 mL |
| 5 mM | 0.4827 mL | 2.4135 mL | 4.8271 mL | 12.0677 mL | |
| H2O | 10 mM | 0.2414 mL | 1.2068 mL | 2.4135 mL | 6.0338 mL |
| 15 mM | 0.1609 mL | 0.8045 mL | 1.6090 mL | 4.0226 mL | |
| 20 mM | 0.1207 mL | 0.6034 mL | 1.2068 mL | 3.0169 mL | |
| 25 mM | 0.0965 mL | 0.4827 mL | 0.9654 mL | 2.4135 mL | |
| 30 mM | 0.0805 mL | 0.4023 mL | 0.8045 mL | 2.0113 mL | |
| 40 mM | 0.0603 mL | 0.3017 mL | 0.6034 mL | 1.5085 mL | |
| 50 mM | 0.0483 mL | 0.2414 mL | 0.4827 mL | 1.2068 mL | |
| 60 mM | 0.0402 mL | 0.2011 mL | 0.4023 mL | 1.0056 mL | |
| 80 mM | 0.0302 mL | 0.1508 mL | 0.3017 mL | 0.7542 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
HLI373 dihydrochloride 関連分類
HY-108640A 関連分類
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