Hydroxy-PP-Me
Based on 1 Customer Validation
Hydroxy-PP-Me is a selective CBR1 inhibitor with an IC50 of 759 nM. Hydroxy-PP-Me can inhibit serum starvation-induced apoptosis. Hydroxy-PP-Me can enhance the cytotoxic effects of Daunorubicin (HY-13062A) and As2O3 on tumor cells. Hydroxy-PP-Me can be used in the research of cancer such as leukemia.
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- Purity: 98.62%
- CAS No.: 833481-77-9
- 화학식: C16H18N4O
- 분자량:282.34
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
IC50: 759 nM (CBR1)[1]
In Vitro
Hydroxy-PP-Me (1-8 μM; 24 h) enhances the cell-killing effect mediated by Daunorubicin (HY-13062A) in A549 cells[1].
Hydroxy-PP-Me (6.3-25 μM; 65 h) inhibits serum starvation-induced apoptosis in A549 cells[1].
Hydroxy-PP-Me (20 μM; 48 h), when used in combination with As2O3 in human myeloid leukemia cell lines (U937, K562, HL-60, NB4), significantly enhances apoptotic cell death[2].
Hydroxy-PP-Me (20 μM; 0-36 h) enhances As2O3-induced ROS production in U937 cells by activating NADPH oxidase[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells treated serum starvation
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Concentration:6.3, 12.5 and 25 μM
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Incubation Time:65 h
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Result:Decreased PI staining in a dose-dependent manner.
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Cell Line:As2O3 treated U937 and K562 cells
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Concentration:20 μM
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Incubation Time:48 h
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Result:Increased the cleaved PARP and caspase-3 levels.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic BALB/c nude mice aged 5-6 weeks old treated U937 cells and As2O3[2]
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Dosage:30 mg/kg
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Administration:Intraperitoneal injection; once every 3 days for 18 days
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Result:Markedly suppressed tumor growth and weight compared with As2O3 alone.
Enhanced expression of apoptotic markers and apoptotic nuclei in tumor specimens.
Chemical Information
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CAS No. 833481-77-9
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Appearance Solid
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분자량 282.34
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화학식 C16H18N4O
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Color Off-white to light yellow
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SMILES
OC1=CC=CC(C2=CN(C(C)C)C3=C2C(NC)=NC=N3)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (354.18 mM; Need ultrasonic; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (8.85 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (8.85 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (281 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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Handling Instructions (2659 KB)
References
[1]. Tanaka M, et al. An unbiased cell morphology-based screen for new, biologically active small molecules. PLoS Biol. 2005 May;3(5):e128. [Content Brief]
[2]. Jang M, et al. Carbonyl reductase 1 offers a novel therapeutic target to enhance leukemia treatment by arsenic trioxide. Cancer Res. 2012 Aug 15;72(16):4214-24. [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. 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 |
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| DMSO | 1 mM | 3.5418 mL | 17.7091 mL | 35.4183 mL | 88.5457 mL |
| 5 mM | 0.7084 mL | 3.5418 mL | 7.0837 mL | 17.7091 mL | |
| 10 mM | 0.3542 mL | 1.7709 mL | 3.5418 mL | 8.8546 mL | |
| 15 mM | 0.2361 mL | 1.1806 mL | 2.3612 mL | 5.9030 mL | |
| 20 mM | 0.1771 mL | 0.8855 mL | 1.7709 mL | 4.4273 mL | |
| 25 mM | 0.1417 mL | 0.7084 mL | 1.4167 mL | 3.5418 mL | |
| 30 mM | 0.1181 mL | 0.5903 mL | 1.1806 mL | 2.9515 mL | |
| 40 mM | 0.0885 mL | 0.4427 mL | 0.8855 mL | 2.2136 mL | |
| 50 mM | 0.0708 mL | 0.3542 mL | 0.7084 mL | 1.7709 mL | |
| 60 mM | 0.0590 mL | 0.2952 mL | 0.5903 mL | 1.4758 mL | |
| 80 mM | 0.0443 mL | 0.2214 mL | 0.4427 mL | 1.1068 mL | |
| 100 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.8855 mL |
Hydroxy-PP-Me Related Classifications
HY-156694 Related Classifications
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