PPA24
Based on 1 Customer Validation
PPA24 is a PP2A activator with a KD of 8.465 μM for PP2ACα. PPA24 induces cancer cell death via apoptosis. PP2ACα induces ROS generation and decreases the level of c-Myc expression. PPA24 can be used to study colorectal cancer (CRC), Folinic acid (HY-17556), 5-Fluorouracil (HY-90006), and Oxaliplatin (HY-17371) (FOLFOX)-resistant CRC, and melanoma cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.09%
- CAS. Nr.: 3035032-77-7
- Formel: C22H27BrClN5S
- Molecular Weight:508.91
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PP2A |
GSK-3α |
GSK-3β |
In Vitro
PPA24 (0.5-50 μM, 48 h) shows cytotoxicity against HCT116, HT29, DLD1, SW480, FOLFOX HCT116 and FOLFOX HT29, with IC50s of 3.95, 6.75, 3.45, 3.64, 2.63 and 3.04 μM, respectively, shows weak cytotoxicity against HaCaT, with IC50 of 10.04 μM[1].
PPA24 (2.5-10 μM, 24 h) induces apoptosis in HCT116, HT29, FOLFOX HCT116, FOLFOX HT29 cells[1].
PPA24 (2.5-5 μM, 6-12 h) stimulates ROS generation in HCT116 cells[1].
PPA24 (2.5-5 μM, 24 h) decreases the level of c-Myc expression in HCT116, FOLFOX HCT116 cells[1].
PPA24 (0.1-10 μM, 48 h) shows a synergistic effect and Gemcitabine (HY-17026) or Cisplatin (HY-17394) with HCT116 cells[1].
PPA24 shows cytotoxicity against SK-MEL-2, SK-MEL-28, A375, Mel1241, and 451Lu cells with IC50s in the range of 5.99-14.45 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HCT116, HT29, FOLFOX HCT116, FOLFOX HT29
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Induced apoptosis.
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Cell Line:HCT116, FOLFOX HCT116
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Concentration:2.5 μM, 5 μM
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Incubation Time:24 h
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Result:Decreased the level of c-Myc expression, did not increase the level of degradation of c-Myc.
Reduced the protein expression level of GSK-3α/β but did not change p-GSK-3α/β (S21/9).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT116 (1.5 × 106) xenografts nude mice model[1]
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Dosage:6 mg/kg, nanoformulation (Nano-PPA24)
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Administration:i.v., three times per week, 23 days
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Result:Inhibited tumor growth with no significant changes in body weight.
Chemical Information
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CAS. Nr. 3035032-77-7
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Appearance Solid
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Molecular Weight 508.91
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Formel C22H27BrClN5S
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Color White to off-white
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SMILES
ClC1=CC=C2C(N(C3=CC=CC=C3S2)CCCC[N+]4(C[N@@](C5)C6)C[N@@]6C[N@@]5C4)=C1.[Br-]
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (196.50 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 (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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (4.91 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.91 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 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protokoll
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Reinheit & Dokumentation
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Data Sheet (279 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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Handling Instructions (2659 KB)
Verweise
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 |
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| DMSO | 1 mM | 1.9650 mL | 9.8249 mL | 19.6498 mL | 49.1246 mL |
| 5 mM | 0.3930 mL | 1.9650 mL | 3.9300 mL | 9.8249 mL | |
| 10 mM | 0.1965 mL | 0.9825 mL | 1.9650 mL | 4.9125 mL | |
| 15 mM | 0.1310 mL | 0.6550 mL | 1.3100 mL | 3.2750 mL | |
| 20 mM | 0.0982 mL | 0.4912 mL | 0.9825 mL | 2.4562 mL | |
| 25 mM | 0.0786 mL | 0.3930 mL | 0.7860 mL | 1.9650 mL | |
| 30 mM | 0.0655 mL | 0.3275 mL | 0.6550 mL | 1.6375 mL | |
| 40 mM | 0.0491 mL | 0.2456 mL | 0.4912 mL | 1.2281 mL | |
| 50 mM | 0.0393 mL | 0.1965 mL | 0.3930 mL | 0.9825 mL | |
| 60 mM | 0.0327 mL | 0.1637 mL | 0.3275 mL | 0.8187 mL | |
| 80 mM | 0.0246 mL | 0.1228 mL | 0.2456 mL | 0.6141 mL | |
| 100 mM | 0.0196 mL | 0.0982 mL | 0.1965 mL | 0.4912 mL |
PPA24 Related Classifications
HY-163828 Related Classifications
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