KEA1-97
Based on 1 Customer Validation
KEA1-97 is a selective Thioredoxin-caspase 3 interaction disruptor (IC50=10 μM). KEA1-97 disrupts the interaction of thioredoxin with caspase 3, activates caspases, and induces apoptosis without affecting thioredoxin activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.05%
- No. CAS: 2138882-71-8
- Fòrmula: C15H9Cl2FN4
- Peso molecular:335.16
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Almacenamiento:
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Caspase 3 10 μM (IC50) |
Thioredoxin 10 μM (IC50) |
In Vitro
KEA1-97 (100 μM; 231MFP cells) impaires thioredoxin pulldown of caspase 3[1].
KEA1-97 (10 μM; 48 hours; 231MFP cells) impaires 231MFP serum-free cell proliferation[1].
KEA1-97 (10 μM; 0~12 hours; 231MFP cells) activates caspase 3/7 and induces apoptotic cell death[1].
KEA1-97 (231MFP cells) resistants to survival and proliferation impairments[1].
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:231MFP cells
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Concentration:100 μM
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Incubation Time:
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Result:Impaired thioredoxin pulldown of caspase 3.
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Cell Line:231MFP cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Impaired 231MFP serum-free cell proliferation.
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Cell Line:231MFP cells
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Concentration:10 μM
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Incubation Time:0~12 h
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Result:Activated caspase 3/7 and induced apoptotic cell death.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immune-deficient SCID mice
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Dosage:5 mg/kg
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Administration:I.p.; 50 days
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Result:Attenuated tumor xenograft growth.
Chemical Information
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No. CAS 2138882-71-8
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Appearance Solid
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Peso molecular 335.16
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Fòrmula C15H9Cl2FN4
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Color White to light yellow
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SMILES
ClC1=NC(Cl)=NC(NC2=CC=C(C=C2)C3=CC=C(C=C3)F)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (298.36 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.
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.
Protocolo
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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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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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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
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9836 mL | 14.9182 mL | 29.8365 mL | 74.5912 mL |
| 5 mM | 0.5967 mL | 2.9836 mL | 5.9673 mL | 14.9182 mL | |
| 10 mM | 0.2984 mL | 1.4918 mL | 2.9836 mL | 7.4591 mL | |
| 15 mM | 0.1989 mL | 0.9945 mL | 1.9891 mL | 4.9727 mL | |
| 20 mM | 0.1492 mL | 0.7459 mL | 1.4918 mL | 3.7296 mL | |
| 25 mM | 0.1193 mL | 0.5967 mL | 1.1935 mL | 2.9836 mL | |
| 30 mM | 0.0995 mL | 0.4973 mL | 0.9945 mL | 2.4864 mL | |
| 40 mM | 0.0746 mL | 0.3730 mL | 0.7459 mL | 1.8648 mL | |
| 50 mM | 0.0597 mL | 0.2984 mL | 0.5967 mL | 1.4918 mL | |
| 60 mM | 0.0497 mL | 0.2486 mL | 0.4973 mL | 1.2432 mL | |
| 80 mM | 0.0373 mL | 0.1865 mL | 0.3730 mL | 0.9324 mL | |
| 100 mM | 0.0298 mL | 0.1492 mL | 0.2984 mL | 0.7459 mL |
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