PPIA-IN-1
Based on 1 Customer Validation
PPIA-IN-1 is a PPIA inhibitor with a Kd value of 0.52 μM. PPIA-IN-1 inhibits the PPIA/MAPK signaling pathway to exert antiproliferative activity. PPIA-IN-1 induces G0/G1 cell cycle arrest in cancer cells. PPIA-IN-1 upregulates the expression of Bax and caspase-3, downregulates Bcl-2 expression, and induces apoptosis in cancer cells. PPIA-IN-1 induces increased ROS levels, DNA damage, endoplasmic reticulum stress, and mitochondrial dysfunction in cancer cells. PPIA-IN-1 exhibits antitumor activity in a mouse colon cancer xenograft model. PPIA-IN-1 can be used for the research of colorectal cancer.
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- Pureté : 96.90%
- CAS No.: 3077886-94-0
- Formule: C23H21Cl2FN4O7
- Masse moléculaire:555.34
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
PPIA-IN-1 (Compound 20b) potently inhibits the proliferation of HeLa, HCT116, MCF-7, SW480, CT26, Panc-1 and HepG-2 cells, with IC50 values of 0.69, 0.51, 1.19, 2.59, 0.86, 3.31 and 2.16 μM[1].
PPIA-IN-1 (0-1.2 μM; 24 h) reduces the colony-forming ability of HCT116 cells and inhibits cell migration and invasion[1].
PPIA-IN-1 (0-1.2 μM; 48 h) dose-dependently arrests HCT116 cells at the G0/G1 phase and downregulates the expression of cyclin A2 and CDK4[1].
PPIA-IN-1 (0-1.2 μM; 48 h) induces apoptosis in HCT116 cells, upregulates the expression of Bax and caspase-3, and downregulates the expression of Bcl-2 protein[1].
PPIA-IN-1 (0-1.2 μM; 48 h) increases the intracellular ROS level in HCT116 cells[1].
PPIA-IN-1 (0-1.2 μM; 48 h) inhibits DNA synthesis and proliferation of HCT116 cells, induces cellular DNA damage, and upregulates the expression of γ-H2AX and p53[1].
PPIA-IN-1 (0.3-1.2 μM; 48 h) dose-dependently activates endoplasmic reticulum stress and upregulates the expression of PERK, ATF4 and CHOP in 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:HCT116 cells
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Concentration:0 μM, 0.3 μM, 0.6 μM, 1.2 μM
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Incubation Time:24 h
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Result:Inhibited scratch wound closure by HCT116 cells in a dose-dependent manner.
Caused significant reductions in migration at all tested concentrations compared to the control group.
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Cell Line:HCT116 cells
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Concentration:0 μM, 0.3 μM, 0.6 μM, 1.2 μM
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Incubation Time:48 h
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Result:Caused a dose-dependent increase in the percentage of HCT116 cells in the G0/G1 phase.
Induced a dose-dependent decrease in the percentage of cells in the S and G2/M phases.
Downregulated the expression of cell cycle-related proteins cyclin A2 and CDK4 in a dose-dependent manner.
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Cell Line:HCT116 cells
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Concentration:0 μM, 0.3 μM, 0.6 μM, 1.2 μM
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Incubation Time:48 h
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Result:Induced apoptosis in HCT116 cells in a dose-dependent manner, as shown by increased Annexin V-positive cells.
Upregulated the expression of pro-apoptotic proteins Bax and cleaved caspase-3 in a dose-dependent manner.
Downregulated the expression of anti-apoptotic protein Bcl-2 in a dose-dependent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (22 g, 3 male and 3 female per group, CT26 colon cancer cells injected subcutaneously to form xenograft tumors)[1]
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Dosage:15 mg/kg; 45 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Showed significant dose-dependent inhibition of tumor growth compared to the vehicle group.
Reduced tumor weight and volume in a dose-dependent manner, with 45 mg/kg having greater effect than 15 mg/kg.
Caused no significant changes in body weight, unlike 5-FU (HY-90006) and CsA (HY-B0579).
Increased necrosis regions in tumor tissue as revealed by H&E staining.
Caused no obvious injury or abnormality in major organs.
Markedly decreased Ki67 protein levels in tumor tissue.
- RNA extraction experimental
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- ROS/oxidative-stress fluorescent staining
- Protocol for Cell Cycle
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Mitochondrial membrane-potential and mitochondrial mass staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Genotoxicity/Mutagenicity Study
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 3077886-94-0
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Appearance Solid
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Masse moléculaire 555.34
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Formule C23H21Cl2FN4O7
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Color White to off-white
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SMILES
O=C(C1(C(OCC)=O)OC(C2=CC=CC=C2F)N3C1N(C(C(OC)=O)=C)C4=NC(Cl)=NC(Cl)=C34)OCC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (180.07 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 (protect from light). 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 (protect from light). 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 (4.50 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureté et documentation
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Fiche technique (289 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 (protect from light). 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 | 1.8007 mL | 9.0035 mL | 18.0070 mL | 45.0175 mL |
| 5 mM | 0.3601 mL | 1.8007 mL | 3.6014 mL | 9.0035 mL | |
| 10 mM | 0.1801 mL | 0.9003 mL | 1.8007 mL | 4.5017 mL | |
| 15 mM | 0.1200 mL | 0.6002 mL | 1.2005 mL | 3.0012 mL | |
| 20 mM | 0.0900 mL | 0.4502 mL | 0.9003 mL | 2.2509 mL | |
| 25 mM | 0.0720 mL | 0.3601 mL | 0.7203 mL | 1.8007 mL | |
| 30 mM | 0.0600 mL | 0.3001 mL | 0.6002 mL | 1.5006 mL | |
| 40 mM | 0.0450 mL | 0.2251 mL | 0.4502 mL | 1.1254 mL | |
| 50 mM | 0.0360 mL | 0.1801 mL | 0.3601 mL | 0.9003 mL | |
| 60 mM | 0.0300 mL | 0.1501 mL | 0.3001 mL | 0.7503 mL | |
| 80 mM | 0.0225 mL | 0.1125 mL | 0.2251 mL | 0.5627 mL | |
| 100 mM | 0.0180 mL | 0.0900 mL | 0.1801 mL | 0.4502 mL |
PPIA-IN-1 Related Classifications
HY-172209 Related Classifications
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